Iminosulfonylurea derivatives and herbicides

ABSTRACT

An iminosulfonylurea derivative of the formula (1) or its salt &lt;IMAGE&gt; (1)  wherein Q is   &lt;IMAGE&gt; Q1  &lt;IMAGE&gt; Q2  &lt;IMAGE&gt; Q3 &lt;IMAGE&gt; Q4  &lt;IMAGE&gt; Q5  &lt;IMAGE&gt; Q6  &lt;IMAGE&gt; Q7  &lt;IMAGE&gt; Q8  or &lt;IMAGE&gt; Q9  wherein the variables are herein below defined, and a herbicidal and and growth control method.

This is a continuation of application Ser. No. 08/170,122 filed on Apr. 15, 1994, now U.S. Pat. No. 5,500,406, which was filed as International Application No. PCT/JP92/00808 on Jun. 25, 1992.

TECHNICAL FIELD

The present invention relates to novel iminosulfonylurea derivatives, and herbicides containing them as active ingredients.

BACKGROUND TECHNIQUE

It is indispensable to use herbicides to protect important crop plants such as rice, wheat, corn, soybean, cotton and sugar beet from weeds and thereby to increase the harvest. Especially in recent years, a selective herbicide is desired which is capable of selectively killing weeds without showing any phytotoxicity against crop plants when applied to the foliages of crop plants and weeds simultaneously in a field where such useful crop plants and weeds are coexistent. Further, with a view to avoiding environmental pollution and reducing the costs for transportation and application, researches and developments have been conducted for many years for compounds having high herbicidal effects at low doses. Some of the compounds having such properties are presently used as selective herbicides. However, there still exists a need for better new compounds having such properties.

As the prior art showing a chemical structure similar to that of the compounds of the present invention, Japanese Unexamined Patent Publication No. 15962/1983, No. 103371/1983, No. 126859/1983, No. 48973,1985, No. 214785/1985, No. 134377/1986, No. 151577/1989, No. 45473/1990, No. 91060/1990, No. 7284/1991 and No. 68562/1991, and U.S. Pat. Nos. 4,559,081, 4,592,776, 4,602939, 4,622,065, 4,666,508, 4,696,695 and 4,741,762, disclose compounds having sulfonylurea bonded to a nitrogen atom. However, compounds having sulfonylurea bonded to a nitrogen atom of an imino structure like the compounds of the present invention have not been known at all, and they are novel compounds.

DISCLOSURE OF THE INVENTION

The present inventors have conducted extensive researches over years to develop selective herbicides for important crop plants and have studied herbicidal properties of many compounds with an aim to find out compounds having higher herbicidal activities as well as selectivity. As a result, it has been found that an iminosulfonylurea derivative of the formula (1) or an agriculturally suitable salt thereof: ##STR3## wherein in Q1, Q2 and Q5, E is a sulfur atom, an oxygen atom or a nitrogen atom mono-substituted by an optional substituent other than a hydrogen atom; in Q6, Q7 and Q8, J is a sulfur atom or an oxygen atom; in Q1 to Q8, a nitrogen atom in the ring of Q is substituted by an optional substituent other than a hydrogen atom, and a carbon atom in the ring of Q may be substituted by an optional substituent; and in Q9, the sulfur atom and the nitrogen atom on the carbon atom to which the imino group of Q is bonded, are substituted by optional substituents other than hydrogen atoms, wherein Q is preferably ##STR4##

R^(a1) is a C₁₋₈ alkyl group, a C₃₋₇ cycloalkyl group, a C₁₋₆ alkyl group substituted by a C₃₋₇ cycloalkyl group, a C₃₋₇ cycloalkenyl group, a C₁₋₆ alkyl group substituted by a C₃₋₇ cycloalkenyl group, a C₂₋₈ alkenyl group, a C₂₋₈ alkynyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkoxy group, a C₁₋₆ alkyl group substituted by a C₂₋₆ alkenyloxy group, a C₁₋₆ alkyl group substituted by a C₂₋₆ alkynyloxy group, a C₁₋₆ alkyl group substituted by a mono-, di- or poly-halogeno C₁₋₆ alkoxy group, a C₁₋₆ alkyl group substituted by a mono-, di- or poly-halogeno C₂₋₆ alkenyloxy group, a C₁₋₆ alkyl group substituted by a mono-, di- or poly-halogeno C₂₋₆ alkynyloxy group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylthio group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylsulfinyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylsulfonyl group, a mono-, di- or poly-halogeno C₁₋₈ alkyl group, a mono-, di- or poly-halogeno C₂₋₈ alkenyl group, a mono-, di- or poly-halogeno C₂₋₈ alkynyl group, a C₁₋₆ alkyl group substituted by a cyano group, a C₂₋₆ alkenyl group substituted by a cyano group, a C₂₋₆ alkynyl group substituted by a cyano group, a C₁₋₆ alkyl group substituted by a nitro group, a C₂₋₆ alkenyl group substituted by a nitro group, a C₂₋₆ alkynyl group substituted by a nitro group, a C₁₋₆ alkyl group substituted by a C₂₋₇ alkoxycarbonyl group, a C₂₋₆ alkenyl group substituted by a C₂₋₇ alkoxycarbonyl group, a C₂₋₆ alkynyl group substituted by a C₂₋₇ alkoxycarbonyl group, a C₁₋₆ alkyl group substituted by a C₂₋₇ alkylcarbonyl group, a C₁₋₆ alkyl group substituted by a mono-, di- or poly-halogeno C₂₋₇ alkylcarbonyl group, a C₁₋₆ alkyl group substituted by a C₃₋₇ alkenylcarbonyl group, a C₁₋₆ alkyl group substituted by a C₃₋₇ alkynylcarbonyl group, a C₁₋₆ alkyl group substituted by a C₂₋₅ alkylcarbonyl group substituted by a C₁₋₄ alkoxy group, a C₁₋₆ alkyl group substituted by a C₂₋₅ alkylcarbonyl group substituted by a C₁₋₄ alkylthio group, a C₁₋₆ alkyl group substituted by a C₂₋₅ alkylcarbonyl group substituted by a C₁₋₄ alkylsulfinyl group, a C₁₋₆ alkyl group substituted by a C₂₋₅ alkylcarbonyl group substituted by a C₁₋₄ alkylsulfonyl group, a C₂₋₆ alkenyl group substituted by a C₂₋₇ alkylcarbonyl group, a C₂₋₆ alkynyl group substituted by a C₂₋₇ alkylcarbonyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylsulfamoyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkoxysulfamoyl group, a C₁₋₆ alkyl group substituted by a di(C₁₋₃ alkyl)sulfamoyl group, a C₁₋₆ alkyl group substituted by an N-(C₁₋₃ alkyl)-N-(C₁₋₃ alkoxy)sulfamoyl group, a C₁₋₆ alkyl group substituted by a C₂₋₇ alkylcarbamoyl group, a C₁₋₆ alkyl group substituted by a di(C₁₋₃ alkyl)carbamoyl group, a C₁₋₆ alkyl group substituted by a C₂₋₇ alkoxycarbamoyl group, a C₁₋₆ alkyl group substituted by an N-(C₁₋₃ alkyl)-N-(C₁₋₃ alkoxy)carbamoyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylamino group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkoxyamino group, a C₁₋₆ alkyl group substituted by a di(C₁₋₃ alkyl)amino group, a C₁₋₆ alkyl group substituted by an N-(C₁₋₃ alkyl)-N-(C₁₋₃ alkoxy)amino group, a C₁₋₆ alkyl group substituted by an N-(C₂₋₇ alkylcarbonyl)-N-(C₁₋₆ alkyl)amino group, a C₁₋₆ alkyl group substituted by an N-(C₂₋₇ alkylcarbonyl)-N-(C₁₋₆ alkoxy)amino group, a C₁₋₆ alkyl group substituted by an N-(C₁₋₆ alkylsulfonyl)-N-(C₁₋₆ alkyl)amino group, a C₁₋₆ alkyl group substituted by an N-(C₁₋₆ alkylsulfonyl)-N-(C₁₋₆ alkoxy)amino group, a phenyl group (provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenyl group (provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₂₋₇ alkenyl group substituted by a phenyl group (provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₂₋₆ alkynyl group substituted by a phenyl group (provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenoxy group (provided that such a phenoxy group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenylthio group (provided that such a phenylthio group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenylsulfinyl group (provided that such a phenylsulfinyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenylsulfonyl group (provided that such a phenylsulfonyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a benzyloxy group (provided that the phenyl group of such a benzyloxy group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a benzylthio group (provided that the phenyl group of such a benzylthio group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a benzylsulfinyl group (provided that the phenyl group of such a benzylsulfinyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a benzylsulfonyl group (provided that the phenyl group of such a benzylsulfonyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenylcarbonyl group (provided that such a phenylcarbonyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a benzylcarbonyl group (provided that the phenyl group of such a benzylcarbonyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ akloxycarbonyl group), a C₁₋₆ alkyl group substituted by an amino group substituted by a C₁₋₄ alkylsulfonyl group, or a C₁₋₆ alkyl group substituted by an amino group substituted by a C₂₋₄ alkylcarbonyl group,

each of R^(a2) and R^(a3) which are independent of each other, is a hydrogen atom, a C₁₋₆ alkyl group, a mono-, di- or poly-halogeno C₁₋₆ alkyl group, a C₁₋₆ alkoxy group, a mono-, di or poly-halogeno C₁₋₆ alkoxy group, a C₁₋₆ alkylthio group, a C₁₋₆ alkylsulfinyl group, a C₁₋₆ alkylsulfonyl group, a C₂₋₇ alkoxycarbonyl group, a C₂₋₇ alkylcarbonyl group, a halogen atom, a nitro group, a cyano group, or a phenyl group (provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group),

each of R^(a4) and R^(a5) which are independent of each other, is a hydrogen atom, a C₁₋₈ alkyl group, a C₂₋₈ alkenyl group, a C₂₋₈ alkynyl group, or a phenyl group (provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group),

R^(a6) is a C₁₋₈ alkyl group, a C₂₋₈ alkenyl group, a C₂₋₈ alkynyl group or a phenyl group (provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group),

R^(b1) is a C₁₋₈ alkyl group, a C₃₋₇ cycloalkyl group, a C₁₋₆ alkyl group substituted by a C₃₋₇ cycloalkyl group, a C₃₋₇ cycloalkenyl group, a C₁₋₆ alkyl group substituted by a C₃₋₇ cycloalkenyl group, a C₂₋₈ alkenyl group, a C₂₋₈ alkynyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkoxy group, a C₁₋₆ alkyl group substituted by a C₂₋₇ alkenyloxy group, a C₁₋₆ alkyl group substituted by a C₂₋₆ alkynyloxy group, a C₁₋₆ alkyl group substituted by a mono-, di or poly-halogeno C₁₋₆ alkoxy group, a C₁₋₆ alkyl group substituted by a mono-, di- or poly-halogeno C₂₋₆ alkenyloxy group, a C₁₋₆ alkyl group substituted by a mono-, di- or poly-halogeno C₂₋₆ alkynyloxy group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylthio group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylsulfinyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylsulfonyl group, a mono-, di- or poly-halogeno C₁₋₈ alkyl group, a mono-, di or poly-halogeno C₂₋₈ alkenyl group, a mono-, di- or poly-halogeno C₂₋₈ alkynyl group, a C₁₋₆ alkyl group substituted by a cyano group, a C₂₋₆ alkenyl group substituted by a cyano group, a C₂₋₆ alkynyl group substituted by a cyano group, a C₁₋₆ alkyl group substituted by a nitro group, a C₂₋₆ alkenyl group substituted by a nitro group, a C₂₋₆ alkynyl group substituted by a nitro group, a C₁₋₆ alkyl group substituted by a C₂₋₇ alkoxycarbonyl group, a C₂₋₆ alkenyl group substituted by a C₂₋₇ alkoxycarbonyl group, a C₂₋₆ alkynyl group substituted by a C₂₋₇ alkoxycarbonyl group, a C₁₋₆ alkyl group substituted by a C₂₋₇ alkylcarbonyl group, a C₁₋₆ alkyl group substituted by a mono-, di- or poly-halogeno C₂₋₇ alkylcarbonyl group, a C₁₋₆ alkyl group substituted by a C₃₋₇ alkenylcarbonyl group, a C₁₋₆ alkyl group substituted by a C₃₋₇ alkynylcarbonyl group, a C₁₋₆ alkyl group substituted by a C₂₋₅ alkylcarbonyl group substituted by a C₁₋₄ alkoxy group, a C₁₋₆ alkyl group substituted by a C₂₋₅ alkylcarbonyl group substituted by a C₁₋₄ alkylthio group, a C₁₋₆ alkyl group substituted by a C₂₋₅ alkylcarbonyl group substituted by a C₁₋₄ alkylsulfinyl group, a C₁₋₆ alkyl group substituted by a C₂₋₅ alkylcarbonyl group substituted by a C₁₋₄ alkylsulfonyl group, a C₂₋₆ alkenyl group substituted by a C₂₋₇ alkylcarbonyl group, a C₂₋₆ alkynyl group substituted by a C₂₋₇ alkylcarbonyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylsulfamoyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkoxysulfamoyl group, a C₁₋₆ alkyl group substituted by a di(C₁₋₃ alkyl)sulfamoyl group, a C₁₋₆ alkyl group substituted by an N-(C₁₋₃ alkyl)-N-(C₁₋₃ alkoxy)sulfamoyl group, a C₁₋₆ alkyl group substituted by a C₂₋₇ alkylcarbamoyl group, a C₁₋₆ alkyl group substituted by a di(C₁₋₃ alkyl)carbamoyl group, a C₁₋₆ alkyl group substituted by a C₂₋₇ alkoxycarbamoyl group, a C₁₋₆ alkyl group substituted by an N-(C₁₋₃ alkyl)-N-(C₁₋₃ alkoxy)carbamoyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylamino group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkoxyamino group, a C₁₋₆ alkyl group substituted by a di(C₁₋₃ alkyl)amino group, a C₁₋₆ alkyl group substituted b an N-(C₁₋₃ alkyl)-N-(C₁₋₃ alkoxy)amino group, a C₁₋₆ alkyl group substituted by an N-(C₂₋₇ alkylcarbonyl)-N-(C₁₋₆ alkyl)amino group, a C₁₋₆ alkyl group substituted by an N-(C₂₋₇ alkylcarbonyl)-N-(C₁₋₆ alkoxy)amino group, a C₁₋₆ alkyl group substituted by an N-(C₁₋₆ alkylsulfonyl)-N-(C₁₋₆ alkyl)amino group, a C₁₋₆ alkyl group substituted by an N-(C₁₋₆ alkylsulfonyl)-N-(C₁₋₆ alkoxy)amino group, a phenyl group (provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenyl group (provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₂₋₇ alkenyl group substituted by a phenyl group (provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₂₋₆ alkynyl group substituted by a phenyl group (provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenoxy group (provided that such a phenoxy group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenylthio group (provided that such a phenylthio group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenylsulfinyl group (provided that such a phenylsulfinyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenylsulfonyl group (provided that such a phenylsulfonyl group may be substituted bone or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a benzyloxy group (provided that the phenyl group of such a benzyloxy group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a benzylthio group (provided that the phenyl group of such a benzylthio group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a benzylsulfinyl group (provided that the phenyl group of such a benzylsulfinyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a benzylsulfonyl group (provided that the phenyl group of such a benzylsulfonyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenylcarbonyl group (provided that such a phenylcarbonyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a benzylcarbonyl group (provided that the phenyl group of such a benzylcarbonyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by an amino group substituted by a C₁₋₄ alkylsulfonyl group, or a C₁₋₆ alkyl group substituted by an amino group substituted by a C₂₋₄ alkylcarbonyl group,

R^(b2) is a hydrogen atom, a C₁₋₆ alkyl group, a mono-, di- or poly-halogeno C₁₋₆ alkyl group, a C₁₋₆ alkoxy group, a mono-, di- or poly-halogeno C₁₋₆ alkoxy group, a C₁₋₆ alkylthio group, a C₁₋₆ alkylsulfinyl group, a C₁₋₆ alkylsulfonyl group, a C₂₋₇ alkoxycarbonyl group, a C₂₋₇ alkylcarbonyl group, a halogen atom, a nitro group, a cyano group, or a phenyl group (provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group),

R^(b3) is a C₁₋₆ alkyl group, a C₂₋₆ alkenyl group or a C₂₋₆ alkynyl group,

R^(b4) is a hydrogen atom, or a C₁₋₆ alkyl group,

R^(b5) is a hydrogen atom, or a C₁₋₆ alkyl group,

R^(c1) is a C₁₋₈ alkyl group, a C₃₋₇ cycloalkyl group, a C₁₋₆ alkyl group substituted by a C₃₋₇ cycloalkyl group, a C₃₋₇ cycloalkenyl group, a C₁₋₆ alkyl group substituted by a C₃₋₇ cycloalkenyl group, a C₂₋₈ alkenyl group, a C₂₋₈ alkynyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkoxy group, a C₁₋₆ alkyl group substituted by a C₂₋₆ alkenyloxy group, a C₁₋₆ alkyl group substituted by a C₂₋₆ alkynyloxy group, a C₁₋₆ alkyl group substituted by a mono-, di- or poly-halogeno C₁₋₆ alkoxy group, a C₁₋₆ alkyl group substituted by a mono-, di- or poly-halogeno C₂₋₆ alkenyloxy group, a C₁₋₆ alkyl group substituted by a mono-, di- or poly-halogeno C₂₋₆ alkynyloxy group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylthio group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylsulfinyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylsulfonyl group, a mono-, di- or poly-halogeno C₁₋₈ alkyl group, a mono-, di- or poly-halogeno C₂₋₈ alkenyl group, a mono-, di- or poly-halogeno C₂₋₈ alkynyl group, a C₁₋₆ alkyl group substituted by a cyano group, a C₂₋₆ alkenyl group substituted by a cyano group, a C₂₋₆ alkynyl group substituted by a cyano group, a C₁₋₆ alkyl group substituted by a nitro group, a C₂₋₆ alkenyl group substituted by a nitro group, a C₂₋₆ alkynyl group substituted by a nitro group, a C₁₋₆ alkyl group substituted by a C₂₋₇ alkoxycarbonyl group, a C₂₋₆ alkenyl group substituted by a C₂₋₇ alkoxycarbonyl group, a C₂₋₆ alkynyl group substituted by a C₂₋₇ alkoxycarbonyl group, a C₁₋₆ alkyl group substituted by a C₂₋₇ alkylcarbonyl group, a C₁₋₆ alkyl group substituted by a mono-, di- or poly-halogeno C₂₋₇ alkylcarbonyl group, a C₁₋₆ alkyl group substituted by a C₃₋₇ alkenylcarbonyl group, a C₁₋₆ alkyl group substituted by a C₃₋₇ alkynylcarbonyl group, a C₁₋₆ alkyl group substituted by a C₂₋₅ alkylcarbonyl group substituted by a C₁₋₄ alkoxy group, a C₁₋₆ alkyl group substituted by a C₂₋₅ alkylcarbonyl group substituted by a C₁₋₄ alkylthio group, a C₁₋₆ alkyl group substituted by a C₂₋₅ alkylcarbonyl group substituted by a C₁₋₄ alkylsulfinyl group, a C₁₋₆ alkyl group substituted by a C₂₋₅ alkylcarbonyl group substituted by a C₁₋₄ alkylsulfonyl group, a C₂₋₆ alkenyl group substituted by a C₂₋₇ alkylcarbonyl group, a C₂₋₆ alkynyl group substituted by a C₂₋₇ alkylcarbonyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylsulfamoyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkoxysulfamoyl group, a C₁₋₆ alkyl group substituted by a di(C₁₋₃ alkyl)sulfamoyl group, a C₁₋₆ alkyl group substituted by an N-(C₁₋₃ alkyl)-N-(C₁₋₃ alkoxy)sulfamoyl group, a C₁₋₆ alkyl group substituted by a C₂₋₇ alkylcarbamoyl group, a C₁₋₆ alkyl group substituted by a di(C₁₋₃ alkyl)carbamoyl group, a C₁₋₆ alkyl group substituted by a C₂₋₇ alkoxycarbamoyl group, a C₁₋₆ alkyl group substituted by an N-(C₁₋₃ alkyl)-N-(C₁₋₃ alkoxy)carbamoyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylamino group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkoxyamino group, a C₁₋₆ alkyl group substituted by a di(C₁₋₃ alkyl)amino group, a C₁₋₆ alkyl group substituted by an N-(C₁₋₃ alkyl)-N-(C₁₋₃ alkoxy)amino group, a C₁₋₆ alkyl group substituted by an N-(C₂₋₇ alkylcarbonyl)-N-(C₁₋₆ alkyl)amino group, a C₁₋₆ alkyl group substituted by an N-(C₂₋₇ alkylcarbonyl)-N-(C₁₋₆ alkoxy)amino group, a C₁₋₆ alkyl group substituted by an N-(C₁₋₆ alkylsulfonyl)-N-(C₁₋₆ alkyl)amino group, a C₁₋₆ alkyl group substituted by an N-(C₁₋₆ alkylsulfonyl)-N-(C₁₋₆ alkoxy)amino group, a phenyl group (provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenyl group (provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₂₋₇ alkenyl group substituted by a phenyl group (provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₂₋₆ alkynyl group substituted by a phenyl group (provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenoxy group (provided that such a phenoxy group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenylthio group (provided that such a phenylthio group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenylsulfinyl group (provided that such a phenylsulfinyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenylsulfonyl group (provided that such a phenylsulfonyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a benzyloxy group (provided that the phenyl group of such a benzyloxy group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a benzylthio group (provided that the phenyl group of such a benzylthio group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a benzylsulfinyl group (provided that the phenyl group of such a benzylsulfinyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a benzylsulfonyl group (provided that the phenyl group of such a benzylsulfonyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenylcarbonyl group (provided that such a phenylcarbonyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a benzylcarbonyl group (provided that the phenyl group of such a benzylcarbonyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by an amino group substituted by a C₁₋₄ alkylsulfonyl group, or a C₁₋₆ alkyl group substituted by an amino group substituted by a C₂₋₄ alkylcarbonyl group,

each of R^(c2), R^(c3), R^(c4), R^(c5), R^(c6), R^(c11) and R^(c12) which are independent of one another, is a hydrogen atom, a C₁₋₈ alkyl group, a C₂₋₈ alkenyl group, a C₂₋₈ alkynyl group, or a phenyl group (provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group),

each of R^(c7), R^(c8), R^(c9), R^(c10), R^(c13) and R^(c14) which are independent of one another, is a hydrogen atom, a C₁₋₆ alkyl group, a mono-, di- or poly-halogeno C₁₋₆ alkyl group, a C₁₋₆ alkoxy group, a mono, di- or poly-halogeno C₁₋₆ alkoxy group, a C₁₋₆ alkylthio group, a C₁₋₆ alkylsulfinyl group, a C₁₋₆ alkylsulfonyl group, a C₂₋₇ alkoxycarbonyl group, a C₂₋₇ alkylcarbonyl group, a halogen atom, a nitro group, a cyano group, or a phenyl group (provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group),

R^(d1) is a C₁₋₈ alkyl group, a C₃₋₇ cycloalkyl group, a C₁₋₆ alkyl group substituted by a C₃₋₇ cycloalkyl group, a C₃₋₇ cycloalkenyl group, a C₁₋₆ alkyl group substituted by a C₃₋₇ cycloalkenyl group, a C₂₋₈ alkenyl group, a C₂₋₈ alkynyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkoxy group, a C₁₋₆ alkyl group substituted by a C₂₋₆ alkenyloxy group, a C₁₋₆ alkyl group substituted by a C₂₋₆ alkynyloxy group, a C₁₋₆ alkyl group substituted b a mono-, di or poly-halogeno C₁₋₆ alkoxy group, a C₁₋₆ alkyl group substituted by a mono-, di- or poly-halogeno C₂₋₆ alkenyloxy group, a C₁₋₆ alkyl group substituted by a mono-, di- or poly-halogeno C₂₋₆ alkynyloxy group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylthio group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylsulfinyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylsulfonyl group, a mono-, di- or poly-halogeno C₁₋₈ alkyl group, a mono-, di- or poly-halogeno C₂₋₈ alkenyl group, a mono-, di- or poly-halogeno C₂₋₈ alkynyl group, a C₁₋₆ alkyl group substituted by a cyano group, a C₂₋₆ alkenyl group substituted by a cyano group, a C₂₋₆ alkynyl group substituted by a cyano group, a C₁₋₆ alkyl group substituted by a nitro group, a C₂₋₆ alkenyl group substituted by a nitro group, a C₂₋₆ alkynyl group substituted by a nitro group, a C₁₋₆ alkyl group substituted by a C₂₋₇ alkoxycarbonyl group, a C₂₋₆ alkenyl group substituted by a C₂₋₇ alkoxycarbonyl group, a C₂₋₆ alkynyl group substituted by a C₂₋₇ alkoxycarbonyl group, a C₁₋₆ alkyl group substituted by a C₂₋₇ alkylcarbonyl group, a C₁₋₆ alkyl group substituted by a mono-, di- or poly-halogeno C₂₋₇ alkylcarbonyl group, a C₁₋₆ alkyl group substituted by a C₃₋₇ alkenylcarbonyl group, a C₁₋₆ alkyl group substituted by a C₃₋₇ alkynylcarbonyl group, a C₁₋₆ alkyl group substituted by a C₂₋₅ alkylcarbonyl group substituted by a C₁₋₄ alkoxy group, a C₁₋₆ alkyl group substituted by a C₂₋₅ alkylcarbonyl group substituted by a C₁₋₄ alkylthio group, a C₁₋₆ alkyl group substituted by a C₂₋₅ alkylcarbonyl group substituted by a C₁₋₄ alkylsulfinyl group, a C₁₋₆ alkyl group substituted by a C₂₋₅ alkylcarbonyl group substituted by a C₁₋₄ alkylsulfonyl group, a C₂₋₆ alkenyl group substituted by a C₂₋₇ alkylcarbonyl group, a C₂₋₆ alkynyl group substituted by a C₂₋₇ alkylcarbonyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylsulfamoyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkoxysulfamoyl group, a C₁₋₆ alkyl group substituted by a di(C₁₋₃ alkyl)sulfamoyl group, a C₁₋₆ alkyl group substituted by an N-(C₁₋₃ alkyl)-N-(C₁₋₃ alkoxy)sulfamoyl group, a C₁₋₆ alkyl group substituted by a C₂₋₇ alkylcarbamoyl group, a C₁₋₆ alkyl group substituted by a di(C₁₋₃ alkyl)carbamoyl group, a C₁₋₆ alkyl group substituted by a C₂₋₇ alkoxycarbamoyl group, a C₁₋₆ alkyl group substituted by an N-(C₁₋₃ alkyl)-N-(C₁₋₃ alkoxy)carbamoyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylamino group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkoxyamino group, a C₁₋₆ alkyl group substituted by a di(C₁₋₃ alkyl)amino group, a C₁₋₆ alkyl group substituted by an N-(C₁₋₃ alkyl)-N-(C₁₋₃ alkoxy)amino group, a C₁₋₆ alkyl group substituted by an N-(C₂₋₇ alkylcarbonyl)-N-(C₁₋₆ alkyl)amino group, a C₁₋₆ alkyl group substituted by an N-(C₂₋₇ alkylcarbonyl)-N-(C₁₋₆ alkoxy)amino group, a C₁₋₆ alkyl group substituted by an N-(C₁₋₆ alkylsulfonyl)-N-(C₁₋₆ alkyl)amino group, a C₁₋₆ alkyl group substituted by an N-(C₁₋₆ alkylsulfonyl)-N-(C₁₋₆ alkoxy)amino group, a phenyl group (provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenyl group (provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₂₋₇ alkenyl group substituted by a phenyl group (provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₂₋₆ alkynyl group substituted by a phenyl group (provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenoxy group (provided that such a phenoxy group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenylthio group (provided that such a phenylthio group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenylsulfinyl group (provided that such a phenylsulfinyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenylsulfonyl group (provided that such a phenylsulfonyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a benzyloxy group (provided that the phenyl group of such a benzyloxy group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a benzylthio group (provided that the phenyl group of such a benzylthio group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a benzylsulfinyl group (provided that the phenyl group of such a benzylsulfinyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a benzylsulfonyl group (provided that the phenyl group of such a benzylsulfonyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenylcarbonyl group (provided that such a phenylcarbonyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, A C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a benzylcarbonyl group (provided that the phenyl group of such a benzylcarbonyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by an amino group substituted by a C₁₋₄ alkylsulfonyl group, or a C₁₋₆ alkyl group substituted by an amino group substituted by a C₂₋₄ alkylcarbonyl group,

each of R^(d2), R^(d3) and R^(d4) which are independent of one another, is a hydrogen atom, a C₁₋₈ alkyl group, a C₂₋₈ alkenyl group, a C₂₋₈ alkynyl group, or a phenyl group (provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group),

R^(d5) is a C₁₋₈ alkyl group, a C₂₋₈ alkenyl group, a C₂₋₈ alkynyl group, or a phenyl group (provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group),

R^(d6) is a C₁₋₈ alkyl group, a C₂₋₈ alkenyl group, a C₂₋₈ alkynyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylthio group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylsulfinyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylsulfonyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkoxy group, a C₁₋₆ alkyl group substituted by a C₂₋₇ alkoxycarbonyl group, a C₁₋₆ alkyl group substituted by a C₂₋₇ alkylcarbonyl group, a C₁₋₆ alkyl group substituted by a cyano group, a phenyl group (provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), or a C₁₋₆ alkyl group substituted by a phenyl group (provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group),

R^(e1) is a C₁₋₈ alkyl group, a C₃₋₇ cycloalkyl group, a C₁₋₆ alkyl group substituted by a C₃₋₇ cycloalkyl group, a C₃₋₇ cycloalkenyl group, a C₁₋₆ alkyl group substituted by a C₃₋₇ cycloalkenyl group, a C₂₋₈ alkenyl group, a C₂₋₈ alkynyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkoxy group, a C₁₋₆ alkyl group substituted b a C₂₋₆ alkenyloxy group, a C₁₋₆ alkyl group substituted by a C₂₋₆ alkynyloxy group, a C₁₋₆ alkyl group substituted by a mono-, di- or poly-halogeno C₁₋₆ alkoxy group, a C₁₋₆ alkyl group substituted b a mono-, di- or poly-halogeno C₂₋₆ alkenyloxy group, a C₁₋₆ alkyl group substituted by a mono-, di- or poly-halogeno C₂₋₆ alkynyloxy group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylthio group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylsulfinyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylsulfonyl group, a mono-, di- or poly-halogeno C₁₋₈ alkyl group, a mono-, di- or poly-halogeno C₂₋₈ alkenyl group, a mono-, di- or poly-halogeno C₂₋₈ alkynyl group, a C₁₋₆ alkyl group substituted by a cyano group, a C₂₋₆ alkenyl group substituted by a cyano group, a C₂₋₆ alkynyl group substituted by a cyano group, a C₁₋₆ alkyl group substituted by a nitro group, a C₂₋₆ alkenyl group substituted by a nitro group, a C₂₋₆ alkynyl group substituted by a nitro group, a C₁₋₆ alkyl group substituted by a C₂₋₇ alkoxycarbonyl group, a C₂₋₆ alkenyl group substituted by a C₂₋₇ alkoxycarbonyl group, a C₂₋₆ alkynyl group substituted by a C₂₋₇ alkoxycarbonyl group, a C₁₋₆ alkyl group substituted by a C₂₋₇ alkylcarbonyl group, a C₁₋₆ alkyl group substituted ba mono-, di- or poly-halogeno C₂₋₇ alkylcarbonyl group, a C₁₋₆ alkyl group substituted by a C₃₋₇ alkenylcarbonyl group, a C₁₋₆ alkyl group substituted by a C₃₋₇ alkynylcarbonyl group, a C₁₋₆ alkyl group substituted by a C₂₋₅ alkylcarbonyl group substituted by a C₁₋₄ alkoxy group, a C₁₋₆ alkyl group substituted by a C₂₋₅ alkylcarbonyl group substituted by a C₁₋₄ alkylthio group, a C₁₋₆ alkyl group substituted by a C₂₋₅ alkylcarbonyl group substituted by a C₁₋₄ alkylsulfinyl group, a C₁₋₆ alkyl group substituted by a C₂₋₅ alkylcarbonyl group substituted by a C₁₋₄ alkylsulfonyl group, a C₂₋₆ alkenyl group substituted by a C₂₋₇ alkylcarbonyl group, a C₂₋₆ alkynyl group substituted by a C₂₋₇ alkylcarbonyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylsulfamoyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkoxysulfamoyl group, a C₁₋₆ alkyl group substituted by a di(C₁₋₃ alkyl)sulfamoyl group, a C₁₋₆ alkyl group substituted by an N-(C₁₋₃ alkyl)-N-(C₁₋₃ alkoxy)sulfamoyl group, a C₁₋₆ alkyl group substituted by a C₂₋₇ alkylcarbamoyl group, a C₁₋₆ alkyl group substituted by a di(C₁₋₃ alkyl)carbamoyl group, a C₁₋₆ alkyl group substituted by a C₂₋₇ alkoxycarbamoyl group, a C₁₋₆ alkyl group substituted by an N-(C₁₋₃ alkyl)-N-(C₁₋₃ alkoxy)carbamoyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylamino group, a C₁₋₆ alkyl group substituted b a C₁₋₆ alkoxyamino group, a C₁₋₆ alkyl group substituted by a di(C₁₋₃ alkyl)amino group, a C₁₋₆ alkyl group substituted by an N-(C₁₋₃ alkyl)-N-(C₁₋₃ alkoxy)amino group, a C₁₋₆ alkyl group substituted by an N-(C₂₋₇ alkylcarbonyl)-N-(C₁₋₆ alkyl)amino group, a C₁₋₆ alkyl group substituted by an N-(C₂₋₇ alkylcarbonyl)-N-(C₁₋₆ alkoxy)amino group, a C₁₋₆ alkyl group substituted by an N-(C₁₋₆ alkylsulfonyl)-N-(C₁₋₆ alkyl)amino group, a C₁₋₆ alkyl group substituted by an N-(C₁₋₆ alkylsulfonyl)-N-(C₁₋₆ alkoxy)amino group, a phenyl group (provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenyl group (provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₂₋₇ alkenyl group substituted by a phenyl group (provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₂₋₆ alkynyl group substituted by a phenyl group (provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenoxy group (provided that such a phenoxy group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenylthio group (provided that such a phenylthio group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenylsulfinyl group (provided that such a phenylsulfinyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenylsulfonyl group (provided that such a phenylsulfonyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl gorup), a C₁₋₆ alkyl group substituted by a benzyloxy group (provided that the phenyl group of such a benzyloxy group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a benzylthio group (provided that the phenyl group of such a benzylthio group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a benzylsulfinyl group (provided that the phenyl group of such a benzylsulfinyl group may be substituted by one of more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group , C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a benzylsulfonyl group (provided that the phenyl group of such a benzylsulfonyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenylcarbonyl group (provided that such a phenylcarbonyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a benzylcarbonyl group (provided that the phenyl group of such a benzylcarbonyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by an amino group substituted by a C₁₋₄ alkylsulfonyl group, or a C₁₋₆ alkyl group substituted by an amino group substituted by a C₂₋₄ alkylcarbonyl group,

each of R^(e2), R^(e3), R^(e6) and R^(e7) which are independent of one another, is a hydrogen atom, a C₁₋₆ alkyl group, a mon-, di- or poly-halogeno C₁₋₆ alkyl group, a C₁₋₆ alkoxy group, a mono-, di- or poly-halogeno C₁₋₆ alkoxy group, a C₁₋₆ alkylthio group, a C₁₋₆ alkylsulfinyl group, a C₁₋₆ alkylsulfonyl group, a C₂₋₇ alkoxycarbonyl group, a C₂₋₇ alkylcarbonyl group, a halogen atom, a nitro group a cyano group, or a phenyl group (provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group),

each of R^(e4), R^(e5), R^(e8), R^(e9) and R^(e10) which are independent of one another, is a hydrogen atom, a C₁₋₈ alkyl group, a C₂₋₈ alkenyl group, a C₂₋₈ alkynyl group, or a phenyl group (provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group),

R^(f1) is a C₁₋₈ alkyl group, a C₃₋₇ cycloalkyl group, a C₁₋₆ alkyl group substituted by a C₃₋₇ cycloalkyl group, a C₃₋₇ cycloalkyenyl group, a C₁₋₆ alkyl group substituted by a C₃₋₇ cycloalkenyl group, a C₂₋₈ alkenyl group, a C₂₋₈ alkynyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkoxy group, a C₁₋₆ alkyl group substituted by a C₂₋₆ alkenyloxy group, a C₁₋₆ alkyl group substituted by a C₂₋₆ alkynyloxy group, a C₋₁₋₆ alkyl group substituted by a mono-, di or poly-halogeno C₁₋₆ alkoxy group, a C₁₋₆ alkyl group substituted by a mono-, di- or poly-halogeno C₂₋₆ alkenyloxy group, a C₁₋₆ alkyl group substituted by a mono-, di- or poly-halogeno C₂₋₆ alkynyloxy group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylthio group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylsulfonyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylsulfonyl group, a mono-, di- or poly-halogeno C₁₋₈ alkyl group, a di - or poly-halogeno C₂₋₈ alkynyl group, a C₁₋₆ alkyl group substituted by a cyano group, a C₂₋₆ alkenyl group substituted by a cyano group, a C₂₋₆ alkynyl group substituted by a cyano group, a C₁₋₆ alkyl group substituted by a nitro group, a C₂₋₆ alkenyl group substituted by a nitro group, a C₂₋₆ alkynyl group substituted by a nitro group, a C₁₋₆ alkyl group substituted by a C₂₋₇ alkoxycarbonyl group, a C₂₋₆ alkenyl group substituted by a C₂₋₇ alkoxycarbonyl group, a C₂₋₆ alkynyl group substituted by a C₂₋₇ alkoxycarbonyl group, a C₁₋₆ alkyl group substituted by a C₂₋₇ alkycarbonyl group, a C₁₋₆ alkyl group substituted by mono-, di- or poly-halogeno C₂₋₇ alkylcarbonyl group, a C₁₋₆ alkyl group substituted by a C₃₋₇ alkenylcarbonyl group, a C₁₋₆ alkyl group substituted by a C₃₋₇ alkynylcarbonyl group, a C₁₋₆ alkyl group substituted by a C₂₋₅ alkylcarbonyl group substituted by a C₁₋₄ alkoxy group, a C₁₋₆ alkyl group substituted by a C₂₋₅ alkylcarbonyl group substituted by a C₁₋₄ alkylthio group, a C₁₋₆ alkyl group substituted by a C₂₋₅ alkylcarbonyl group substituted by a C₁₋₄ alkylsulfinyl group, a C₁₋₆ alkyl group substituted by a C₂₋₅ alkylcarbonyl group substituted by a C₁₋₄ alkylsulfonyl group, a C₂₋₆ alkenyl group substituted by a C₂₋₇ alkylcarbonyl group, a C₂₋₆ alkenyl group substituted by a C₂₋₇ alkylcarbonyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylsulfamoyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkoxysulfamoyl group, a C₁₋₆ alkyl group substituted by a di(C₁₋₃ alkyl)sulfamoyl group, a C₁₋₆ alkyl group substituted by an N-(C₁₋₃ alkyl)-N-(C₁₋₃ alkoxy)sulfamoyl group, a C₁₋₆ alkyl group substituted by a C₂₋₇ alkylcarbamoyl group, a C₁₋₆ alkyl group substituted by a di(C₁₋₃ alkyl)carbamoyl group, a C₁₋₆ alkyl group substituted by a C₂₋₇ alkoxycarbamoyl group, a C₁₋₆ alkyl group substituted by an N-(C₁₋₃ alkyl)-N-(C₁₋₃ alkoxy)carbamoyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylamino group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkoxyamino group, a C₁₋₆ alkyl group substituted by a di(C₁₋₃ alkyl)amino group, a C₁₋₆ alkyl group substituted by an N-(C₁₋₃ alkyl)-N-(C₁₋₃ alkoxy)amino group, a C₁₋₆ alkyl group substituted by an N-(C₂₋₇ alkylcarbonyl)-N-(C₁₋₆ alkyl)amino group, a C₁₋₆ alkyl group substituted by an N-(C₂₋₇ alkylcarbonyl)-N-(C₁₋₆ alkoxy)amino group, a C₁₋₆ alkyl group substituted by an N-(C₁₋₆ alkylsulfonyl)-N-(C₁₋₆ alkyl)amino group, a C₁₋₆ alkyl group substituted by an N-(C₁₋₆ alkylsulfonyl)-N-(C₁₋₆ alkoxy)amino group, a phenyl group (provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenyl group (provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₂₋₇ alkenyl group substituted by a phenyl group (provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₂₋₆ alkynyl group substituted by a phenyl group (provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenoxy group (provided that such a phenoxy group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenylthio group (provided that such a phenylthio group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenylsulfinyl group (provided that such a phenylsulfonyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenylsulfonyl group (provided that such a phenylsulfonyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl gorup), a C₁₋₆ alkyl gorup substituted by a benzyloxy group (provided that the phenyl group of such a benzyloxy group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a benzylthio group (provided that the phenyl group of such a benzylthio group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a benzylsulfinyl group provided that the phenyl group of such a benzylsulfinyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a benzylsulfonyl group (provided that the phenyl group of such a benzylsulfonyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenylcarbonyl group (provided that such a phenylcarbonyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a benzylcarbonyl group (provided that the phenyl group of such a benzylcarbonyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by an amino group substituted by a C₁₋₄ alkylsulfonyl group, or a C₁₋ 6 alkyl group substituted by an amino group substituted by a C₂₋₄ alkylcarbonyl group,

R^(f2) is a C₁₋₈ alkyl group, a C₂₋₈ alkenyl group, a C₂₋₈ alkynyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylthio group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylsulfinyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylsulfonyl, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkoxy group, a C₁₋₆ alkyl group substituted by a C₂₋₇ alkoxycarbonyl group, a C₁₋₆ alkyl group substituted by a C₂₋₇ alkylcarbonyl group, a C₁₋₆ alkyl group substituted by a cyano group, a phenyl group (provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), or a C₁₋₆ alkyl group substituted by a phenyl group (provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group),

each of R^(f3), R^(f4), R^(f7), R^(f8), R^(f11) and R^(f12) which are independent of one another, is a hydrogen atom, a C₁₋₆ alkyl group, a mono-, di- or poly-halogeno C₁₋₆ alkyl group, a C₁₋₆ alkoxy group, a mono-, di or poly-halogeno C₁₋₆ alkoxy group, a C₁₋₆ alkylthio group, a C₁₋₆ alkylsulfinyl group, a C₁₋₆ alkylsulfonyl group, a C₂₋₇ alkoxycarbonyl group, a C₂₋₇ alkylcarbonyl group, a halogen atom, a nitro group, a cyano group, or a phenyl group (provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group),

each of R^(f5), R^(f6), R^(f9), R¹⁰, R^(f13), R^(f14) and R^(f15) which are independent of one another, is a hydrogen atom, a C₁₋₈ alkyl group, a C₂₋₈ alkenyl group, a C₂₋₈ alkynyl group, or a phenyl group (provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group),

R^(g1) is a C₁₋₈ alkyl group, a C₃₋₇ cycloalkyl group, a C₁₋₆ alkyl group substituted by a C₃₋₇ cycloalkyl group, a C₃₋₇ cycloalkenyl group, a C₁₋₆ alkyl group substituted by a C₃₋₇ cycloalkenyl group, a C₂₋₈ alkenyl group, a C₂₋₈ alkynyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkoxy group, a C₁₋₆ alkyl group substituted by a C₂₋₆ alkenyloxy group, a C₁₋₆ alkyl group substituted by a C₂₋₆ alkynyloxy group, a C₁₋₆ alkyl group substituted by a mono-, di- or poly-halogeno C₁₋₆ alkoxy group, a C₁₋₆ alkyl group substituted by a mono-, di or poly-halogeno C₂₋₆ alkenyloxy group, a C₁₋₆ alkyl group substituted by a mono-, di- or poly-halogeno C₂₋₆ alkynyloxy group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylthio group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylsulfinyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylsulfonyl group, a mono-, di- or poly-halogeno C₁₋₈ alkyl group, a mono-, di- or poly-halogeno C₂₋₈ alkenyl group, a mono-, di or poly-halogeno C₂₋₈ alkynyl group, a C₁₋₆ alkyl group substituted by a cyano group, a C₂₋₆ alkenyl group substituted by a cyano group, a C₂₋₆ alkynyl group substituted by a cyano group, a C₁₋₆ alkyl group substituted by a nitro group, a C₂₋₆ alkenyl group substituted by a nitro group, a C₂₋₆ alkynyl group substituted by a nitro group, a C₁₋₆ alkyl group substituted by a C₂₋₇ alkoxycarbonyl group, a C₂₋₆ alkenyl group substituted by a C₂₋₇ alkoxycarbonyl group, a C₂₋₆ alkyl group substituted by a C₂₋₇ alkoxycarbonyl group, a C₁₋₆ alkyl group substituted by a C₂₋₇ alkylcarbonyl group, a C₁₋₆ alkyl group substituted by a mono-, di- or poly-halogeno C₂₋₇ alkylcarbonyl group, a C₁₋₆ alkyl group substituted by a C₃₋₇ alkenylcarbonyl group, a C₁₋₆ alkyl group substituted by a C₃₋₇ alkynylcarbonyl group, a C₁₋₆ alkyl group substituted by a C₂₋₅ alkylcarbonyl group substituted by a C₁₋₄ alkoxy group, a C₁₋₆ alkyl group substituted by a C₂₋₅ alkylcarbonyl group substituted by a C₁₋₄ alkylthio group, a C₁₋₆ alkyl group substituted by a C₂₋₅ alkylcarbonyl group substituted by a C₁₋₄ alkylsulfinyl group, a C₁₋₆ alkyl group substituted by a C₂₋₅ alkylcarbonyl group substituted by a C₁₋₄ alkylsulfonyl group, a C₂₋₆ alkenyl group substituted by a C₂₋₇ alkylcarbonyl group, a C₂₋₆ alkynyl group substituted by a C₂₋₇ alkylcarbonyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylsulfamoyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkoxysulfamoyl group, a C₁₋₆ alkyl group substituted by a di(C₁₋₃ alkyl)sulfamoyl group, a C₁₋₆ alkyl group substituted by an N-(C₁₋₃ alkyl)-N-(C₁₋₃ alkoxy)sulfamoyl group, a C₁₋₆ alkyl group substituted by a C₂₋₇ alkyl carbamoyl group, a C₁₋₆ alkyl group substituted by a di(C₁₋₃ alkyl)carbamoyl group, a C₁₋₆ alkyl group substituted by a C₂₋₇ alkoxycarbamoyl group, a C₁₋₆ alkyl group substituted by an N-(C₁₋₃ alkyl)-N-(C₁₋₃ alkoxy)carbamoyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylamino group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkoxyamino group, a C₁₋₆ alkyl group substituted by a di(C₁₋₃ alkyl)amino group, a C₁₋₆ alkyl group substituted by an N-(C₁₋₃ alkyl)-N-(C₁₋₃ alkoxy)amino group, a C₁₋₆ alkyl group substituted by an N-(C₂₋₇ alkylcarbonyl)-N-(C₁₋₆ alkyl)amino group, a C₁₋₆ alkyl group substituted by an N-(C₂₋₇ alkylcarbonyl)-N-(C₁₋₆ alkoxy)amino group, a C₁₋₆ alkyl group substituted by an N-(C₁₋₆ alkylsulfonyl)-N-(C₁₋₆ alkyl)amino group, a C₁₋₆ alkyl group substituted by an N-(C₁₋₆ alkylsulfonyl)-N-(C₁₋₆ alkoxy)amino group, a C₁₋₆ alkyl group substituted by a phenyl group (provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₂₋₇ alkenyl group substituted by a phenyl group (provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₂₋₆ alkynyl group substituted by a phenyl group (provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenoxy group (provided that such a phenoxy group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkyl group substituted by a phenylthio group (provided that such a phenylthio group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenylsulfinyl group (provided that such a phenylsulfinyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenylsulfonyl group (provided that such a phenylsulfonyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a benzyloxy group (provided that the phenyl group of such a benzyloxy group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a benzylthio group (provided that the phenyl group of such a benzylthio group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a benzylsulfinyl group (provided that the phenyl group of such a benzylsulfinyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a benzylsulfonyl group (provided that the phenyl group of such a benzylsulfonyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenylcarbonyl group (provided that such a phenylcarbonyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group, or a C₁₋₆ alkyl group substituted by a benzylcarbonyl group (provided that the phenyl group of such a benzylcarbonyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group),

each of R^(g2) and R^(g3) which are independent of each other, is a C₁₋₆ alkyl group, a C₂₋₆ alkenyl group, a C₂₋ 6 alkynyl group, a mono-, di or poly-halogeno C₁₋₆ alkyl group, a C₁₋₆ alkoxy group, a C₁₋₆ alkylsulfonyl group, a C₁₋₆ alkylsulfamoyl group, a di(C₁₋₃ alkyl)sulfamoyl group, a C₂₋₇ alkoxycarbonyl group, a C₂₋₇ alkylcarbonyl group, a C₂₋₇ alkylcarbamoyl group, a di(C₁₋₃ alkyl)carbamoyl group, a phenyl group (provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), or a benzyl group (provided that the phenyl group of such a benzyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group),

or R^(g2) and R^(g3) form a saturated 3- to 7-membered heterocyclic ring together with the nitrogen atom to which they are bonded.

X is an oxygen atom or a sulfur atom,

L is a hydrogen atom, a C₁₋₆ alkyl group, a C₂₋₆ alkenyl group or a C₂₋₆ alkynyl group,

G is ##STR5##

A is a CH group, or a nitrogen atom, and

each of B and D which are independent of each other, is a C₁₋₄ alkyl group, a C₁₋₄ alkoxy group, a mono-, di- or poly-halogeno C₁₋₄ alkyl group, a mono-, di or poly-halogeno C₁₋₄ alkoxy group, a halogen atom, a C₁₋₄ alkylamino group, or a di(C₁₋₄ alkyl)amino group, (hereinafter referred to as the compound of the present invention) exhibits remarkably strong herbicidal activities against many weeds in soil treatment, in soil admixing treatment or in foliage treatment and at the same time has a high level of safety for important crop plants such as wheat, corn, cotton, soybean, sugar beet and rice, etc. The present invention has been accomplished on the basis of this discovery.

Examples for the substituents R^(a1), R^(a2), R^(a3), R^(a4), R^(a5), R^(a6), R^(b1), R^(b2), R^(b3), R^(b4), R^(b5), R^(c1), R^(c2), R^(c3), R^(c4), R^(c5), R^(c6), R^(c7), R^(c8), R^(c9), R^(c10), R^(c11), R^(c12), R^(c13), R^(c14), R^(d1), R^(d2), R^(d3), R^(d4), R^(d5), R^(d6), R^(e1), R^(e2), R^(e3), R^(e4), R^(e5), R^(e6), R^(e7), R^(e8), R^(e9), R^(e10), R^(f1), R^(f2), R^(f3), R^(f4), R^(f5), R^(f6), R^(f7), R^(f8), R^(f9), R^(f10), R^(f11), R^(f12), R^(f13), R^(f14), R^(f15), R^(g1), R^(g2), R^(g3) L, B and D of the compound of the present invention are as follows. However, symbols have the following meanings.

Me: methyl group, Et: ethyl group, Pr-n: n-propyl group, Pr-iso: isopropyl group, Bu-N: n-butyl group, Bu-iso: isobutyl group, Bu-sec: sec-butyl group, Bu-tert: tert-butyl group, Pen-n: n-pentyl group, Hex-n: n-hexyl group, Hep-n: n-heptyl group, Pr-cyc: cyclopropyl group, Bu-cyc: cyclobutyl group, Pen-cyc: cyclopentyl group, Hex-cyc: cyclohexyl group, and Ph: phenyl group.

Specific examples for the substituents R^(a1), R^(b1), R^(d1), R^(e1) and R^(f1) of the compound of the present invention

Me, Et, Pr-n, Pr-iso, Bu-N, Bu-iso, Bu-sec, Bu-tert, Pen-n, Hex-n, Hep-n, Pr-cyc, Bu-cyc, Pen-cyc, Hex-cyc, CH₂ Pr-cyc, CH₂ CH₂ Pr-cyc, CHMe-Pr-cyc, CH₂ CHMe-Pr-cyc, CHMe CH₂ Pr-cyc, CH₂ Bu-cyc, CH₂ CH₂ Bu-cyc, CH₂ Pen-cyc, CH₂ Hex-cyc, ##STR6##

CH₂ CH═CH₂, CH₂ CH═CHMe, CH₂ CH═CHEt, CH₂ CH₂ CH═CH₂, CH₂ CH₂ CH═CHMe, CH₂ CH═CMe₂, CHMeCH═CH₂, CH₂ CMe═CH₂, CH₂ CMe═CHMe, CHMeCH═CHMe, CH₂ CMe═CHEt, CH₂ CH₂ CH═CMe₂, CH₂ CMe═CMe₂, CH₂ C.tbd.CH, CH₂ C.tbd.CMe, CH₂ C.tbd.CEt, CH₂ CH₂ C.tbd.CH, CH₂ CH₂ C.tbd.CMe, CHMeC.tbd.CH, CHMeC.tbd.CMe, CH₂ OMe, CH₂ OEt, CH₂ OPr-n, CH₂ OPr-iso, CH₂ CH₂ OMe, CH₂ CH₂ OEt, CH₂ CH₂ OPr-n, CHMe OMe, CHMe OEt, CH₂ CHMe OMe, CH₂ CHMe OEt, CH₂ CH₂ CH₂ OMe, CH₂ CH₂ CH₂ OEt, CH₂ OCH₂ CH═CH₂, CH₂ OCH₂ CH═CHMe, CH₂ CH₂ OC₂ CH═CH₂, CH₂ CH₂ OCH₂ CH═CHMe, CH₂ OCH₂ C.tbd.CH, CH₂ OCH₂ C.tbd.CMe, CH₂ OCHMeC.tbd.CH, CH₂ OCMe₂ C.tbd.CH, CH₂ CH₂ OCH₂ C.tbd.CH, CH₂ CH₂ OCH₂ C.tbd.CMe, CH₂ CH₂ OCHMeC.tbd.CH, CH₂ CH₂ OCMe₂ C.tbd.CH, CH₂ OCHF₂, CH₂ OCF₃, CH₂ OCF₂ CF₂, CH₂ CH₂ OCHF₂, CH₂ CH₂ OCF₃, CH₂ CH₂ OCF₂ CF₃, CH₂ OCH₂ CF₃, CH₂ CH₂ OCH₂ CF₃, CH₂ OCH₂ CHF₂, CH₂ CH₂ OCH₂ CHF₂, CH₂ OCH₂ CH₂ F, CH₂ OCH₂ CH₂ C1, CH₂ OCH₂ CH₂ Br, CH₂ CH₂ OCH₂ CH₂ F, CH₂ CH₂ OCH₂ CH₂ Cl, CH₂ CH₂ OCH₂ CH₂ Br, CH₂ OCH₂ CH═CHCl, CH₂ CH₂ OCH₂ CH═CHCl, CH₂ OCH₂ CH═CHBr, CH₂ CH₂ OCH₂ CH═CHBr, CH₂ OCH₂ CF═CF₂, CH₂ CH₂ OCH₂ CF═CF₂, CH₂ OCH═CHCl, CH₂ CH₂ OCH═CHCl, CH₂ OCF═CF₂, CH₂ CH₂ OCF═CF₂, CH₂ OCF₂ CF═CF₂, CH₂ CH₂ OCF₂ CF═CF₂, CH₂ OCH₂ CH═CH₂, CH₂ CH₂ OCH₂ CH═CF₂, CH₂ OCH₂ CH═CHCF₃, CH₂ CH₂ OCH₂ CH═CHCF₃, CH₂ OCH₂ C.tbd.CI, CH₂ OCH₂ CH₂ C.tbd.CI, CH₂ CH₂ OCH₂ C.tbd.CI, CH₂ OCH₂ C.tbd.CCF₃, CH₂ CH₂ OCH₂ C.tbd.CCF₃, CH₂ OCMe₂ C.tbd.CI, CH₂ CH₂ OCMe₂ C.tbd.CI, CH₂ OCMe₂ C.tbd.CCF₂, CH₂ CH₂ OCMe₂ C.tbd.CCF₃, CH₂ SMe, CH₂ SEt, CH₂ SPr-n, CH₂ CH₂ SMe, CH₂ CH₂ SEt, CH₂ CH₂ SPr-n, CHMe SMe, CHMe SEt, CH₂ CHMe SMe, CH₂ CHMe SEt, CH₂ SOMe, CH₂ SOEt, CH₂ SOPr-n, CH₂ CH₂ SOMe, CH₂ CH₂ SOEt, CH₂ CH₂ SOPr-n, CHMe SOMe, CHMe SOEt, CH₂ CHMe SOMe, CH₂ CHMe SOEt, CH₂ SO₂ Me, CH₂ SO₂ Et, CH₂ SO₂ Pr-n, CH₂ CH₂ SO₂ Me, CH₂ CH₂ SO₂ Et, CH₂ CH₂ SO₂ Pr-n, CHMe SO₂ Me, CHMe SO₂ Et, CH₂ CHMe SO₂ Me, CH₂ CHMe SO₂ Et, CH₂ CH₂ F, CH₂ CHF₂, CH₂ CF₃, CH₂ CH₂ Cl, CH₂ CH₂ Br, CH₂ CCl₃, CH₂ CH₂ CF₃, CH₂ CH₂ CCl₃, CH₂ CH₂ CH₂ F, CH₂ CH₂ CH₂ Cl, CF₂ CF₃, CH₂ CF₂ CF₃, CH₂ CH═CHCl, CH₂ CH═CHBr, CH₂ CH═CF₂, CH₂ CF═CF₂, CH₂ CH═CHCF₃, CH₂ CH═CBrMe, CH₂ CH═CClMe, CH₂ CH═C (CF₃) Me, CF₂ CF═CF₂, CH₂ C.tbd.CI, CH₂ CH₂ C.tbd.CI, CH₂ C.tbd.CCF₃, CH₂ CH₂ C.tbd.CCF₃, CH₂ CN, CH₂ CH₂ CN, CHMe CN, CH₂ CHMe CN, CH₂ CMe₂ CN, CH₂ CH═CHCN, CH₂ CH(CN) CH═CH₂, CH₂ C (CN)═CH₂, CH₂ C (CN)═CHMe, CH₂ CH (CN) C.tbd.CH, CH₂ CH (CN) C.tbd.C-Me, CH (CN) C.tbd.CH, CH₂ NO₂, CH₂ CH₂ NO₂, CH₂ CHMeNO₂, CH₂ CMe₂ NO₂, CH₂ CH₂ CH₂ NO₂, CH₂ CH═CHNO₂, CH₂ CH (NO₂) CH═CH₂, CH₂ C (NO₂)═CH₂, CH₂ C (NO₂)═CHMe, CH₂ CH (NO₂) C.tbd.CH, CH₂ CH (NO₂) C.tbd.CMe, CH₂ CO₂ Me, CH₂ CO₂ Et, CH₂ CO₂ Pr-n, CH₂ CO₂ Or-iso, CH₂ CO₂ Bu-n, CHMe CO₂ Me, CHMe CO₂ Et, CH₂ CH₂ CO₂ Me, CH₂ CH₂ CO₂ Et, CH₂ CHMe CO₂ Me, CH₂ CH₂ CH₂ CO₂ Me, CH₂ CH═CHCO₂ Me, CH₂ CH═CHCO₂ Et, CH₂ CH═CHCO₂ Pr-n, CH₂ CH═CMe CO₂ Me, CH₂ CMe═CHCO₂ Me, CHMeCH═CHCO₂ Me, CHMeCH═CHCO₂ Et, CH₂ CH₂ CH═CHCO₂ Me, CH₂ CH═CHCH₂ CO₂ Me, CH₂ C═CCO₂ Me, CH₂ C.tbd.CCO₂ Et, CH₂ C.tbd.CCO₂ Pr-n, CH₂ CH₂ C.tbd.CCO₂ Me, CH₂ CHMeC.tbd.CCO₂ Me, CH₂ CMe₂ C.tbd.CCO₂ Me, CH₂ C.tbd.CCH₂ CO₂ Me, CH₂ COMe, CH₂ COEt, CH₂ COPr-n, CH₂ CH₂ COMe, CH₂ CH₂ COEt, CH₂ CHMe COMe, CH₂ CMe₂ COMe, CH₂ COCF₃, CH₂ COCCl₃, CH₂ CH₂ COCF₃, CH₂ COCH₂ CF₃, CH₂ COCH₂ CHF₂, CH₂ COCH₂ CHCl₂, CH₂ COCH₂ F, CH₂ COCH₂ Cl, CH₂ COCH₂ Br, CH₂ COCH═CH₂, CH₂ COCH═CHMe, CH₂ COCH₂ CH═CH₂, CH₂ CH₂ COCH═CH₂, CH₂ CH₂ COCH═CHMe, CH₂ COC.tbd.CH, CH₂ COC.tbd.CMe, CH₂ COCH₂ C.tbd.CH, CH₂ CH₂ COC.tbd.CH, CH₂ CH₂ COC.tbd.CMe, CH₂ COCH₂ OMe, CH₂ COCH₂ OEt, CH₂ COCH₂ CH₂ OMe, CH₂ COCH₂ CH₂ OEt, CH₂ CH₂ COCH₂ OMe, CH₂ CH₂ COCH₂ OEt, CH₂ COCH₂ SMe, CH₂ COCH₂ SEt, CH₂ COCH₂ CH₂ SMe, CH₂ COCH₂ CH₂ SEt, CH₂ CH₂ COCH₂ SMe CH₂ CH₂ COCH₂ SEt, CH₂ COCH₂ SOMe, CH₂ COCH₂ SOEt, CH₂ COCH₂ CH₂ SOMe, CH₂ COCH₂ CH₂ SOEt, CH₂ CH₂ COCH₂ SOMe, CH₂ CH₂ COCH₂ SOEt, CH₂ COCH₂ SO₂ Me, CH₂ COCH₂ SO₂ Et, CH₂ COCH₂ CH₂ SO₂ Me, CH₂ COCH₂ CH₂ SO₂ Et, CH₂ CH₂ COCH₂ SO₂ Me, CH₂ CH₂ COCH₂ SO₂ Et, CH₂ CH═CHCOMe, CH₂ CH═CHCOEt, CHMeCH═CHCOMe, CHMeCH═CHCOEt, CH₂ C.tbd.CCOMe, CH₂ C.tbd.CCOEt, CHMeC.tbd.CCOMe, CHMeC.tbd.CCOEt, CH₂ SO₂ NHMe, CH₂ SO₂ NHEt, CH₂ SO₂ NHPr-n, CH₂ CH₂ SO₂ NHMe, CH₂ CH₂ SO₂ NHEt, CH₂ CH₂ SO₂ NHPr-n, CH₂ SO₂ NHOMe, CH₂ SO₂ NHOEt, CH₂ SO₂ NHOPr-n, CH₂ CH₂ SO₂ NHOMe, CH₂ CH₂ SO₂ NHOEt, CH₂ CH₂ SO₂ NHOPr-n, CH₂ SO₂ NMe₂, CH₂ SO₂ NMeEt, CH₂ SO₂ NEt₂, CH₂ CH₂ SO₂ NMe₂, CH₂ CH₂ SO₂ NMeEt, CH₂ CH₂ SO₂ NEt₂, CH₂ SO₂ N (OMe) Me, CH₂ SO₂ N (OMe) Et, CH₂ SO₂ N (OEt)Me, CH₂ CH₂ SO₂ N (OMe) Me, CH₂ CH₂ SO₂ N (OMe) Et, CH₂ CH₂ SO₂ N (OEt) Me, CH₂ SO₂ N (OEt) Et, CH₂ CH₂ SO₂ N (OEt) Et, CH₂ CONHMe, CH₂ CONHEt, CH₂ CONHPr-n, CH₂ CH₂ CONHMe, CH₂ CH₂ CONHEt, CH₂ CH₂ CONHPr-n, CH₂ CONMe₂, CH₂ CONMe Et, CH₂ CONEt₂, CH₂ CH₂ CONMe₂, CH₂ CH₂ CONMe Et, CH₂ CH₂ CONEt₂, CH₂ CONHOMe, CH₂ CONHOEt, CH₂ CONHOPr-n, CH₂ CH₂ CONHOMe, CH₂ CH₂ CONHOEt, CH₂ CH₂ CONHOPr-n, CH₂ CON (OMe) Me, CH₂ CON (OMe) Et, CH₂ CON (OEt) Me, CH₂ CH₂ CON (OMe) Me, CH₂ CH₂ CON (OMe) Et, CH₂ CH₂ CON (OEt) Me, CH₂ CON (OEt) Et, CH₂ CH₂ CON (OEt) Et, CH₂ NHMe, CH₂ NHEt, CH₂ NHPr-n, CH₂ CH₂ NHMe, CH₂ CH₂ NHEt, CH₂ CH₂ NHPr-n, CH₂ CHMe NMHe, CH₂ CHMeNHEt, CH₂ CHMeNHPr-n, CH₂ CH₂ CH₂ NHMe, CH₂ NHOMe, CH₂ NHOEt, CH₂ NHOPr-n, CH₂ CH₂ NHOMe, CH₂ CH₂ NHOEt, CH₂ CH₂ NHOPr-n, CH₂ CHMeNMOMe, CH₂ CHMeNHOEt, CH₂ CHMeNHOPr-n, CH₂ NMe₂, CH₂ NMeEt, CH₂ NMePr-n, CH₂ CH₂ NMe₂, CH₂ CH₂ NMeEt, CH₂ CH₂ NMePr-n, CH₂ NEt₂, CH₂ CH₂ NEt₂, CH₂ N (OMe) Me, CH₂ N (OMe) Et, CH₂ N (OEt) Me, CH₂ N (OEt) Et, CH₂ CH₂ N(OMe) Me, CH₂ CH₂ N (OMe) Et, CH₂ CH₂ N (OEt) Me, CH₂ CH₂ N (OEt)Et, CH₂ NMe COMe, CH₂ NEt COMe, CH₂ NMeCOEt, CH₂ CH₂ NMeCOMe, CH₂ CH₂ NEt COMe, CH₂ CH₂ NMe COEt, CH₂ N (OMe) COMe, CH₂ N (OEt) COMe, CH₂ N (OMe) COEt, CH₂ CH₂ N (OMe) COMe, CH₂ CH₂ N (OEt) COMe, CH₂ CH₂ N (OMe) COEt, CH₂ NMe SO₂ Me, CH₂ NEt SO₂ Me, CH₂ NMe SO₂ Et, CH₂ CH₂ NMe SO₂ Me, CH₂ CH₂ NEt SO₂ Me, CH₂ CH₂ NMe SO₂ Et, CH₂ N (OMe) SO₂ Me, CH₂ N (OEt) SO₂ Me, CH₂ N (OMe) SO₂ Et, CH₂ CH₂ N (OMe) SO₂ Me, CH₂ CH₂ N (OEt) SO₂ Me, CH₂ CH₂ N (OMe) SO₂ Et, CH₂ Ph, CH₂ CH₂ Ph, CH₂ CH₂ CH₂ Ph, CHMePh, CH₂ CHMePh, CH₂ CMe₂ Ph, CH₂ CH═CHPh, CH₂ CH═CMe Ph, CHMeCH═CHPh, CH₂ CMe═CMePh, CHMeCMe═CMePh, CH₂ C.tbd.CPh, CHMeC═CPh, CHMeC.tbd.CPh, CH₂ CMe₂ C.tbd.CPh, CH₂ CH₂ OPh, CH₂ CHMe OPh, CH₂ CMe₂ OPh, CH₂ OPh, CH₂ CH₂ SPh, CH₂ CHMeSPh, CH₂ CMe₂ SPh, CH₂ SPh, CH₂ CH₂ SOPh, CH₂ CHMeSOPh, CH₂ CMe₂ SOPh, CH₂ CH₂ SO₂ Ph, CH₂ CHMeSO₂ Ph, CH₂ CMe ₂ SO₂ Ph, CH₂ OCH₂ Ph, CH₂ CH₂ OCH₂ Ph, CH₂ CHMeOCH₂ Ph, CH₂ SCH₂ Ph, CH₂ CH₂ SCH₂ Ph, CH₂ CHMeSCH₂ Ph, CH₂ SOCH₂ Ph, CH₂ CH₂ SOCH₂ Ph, CH₂ CHMeSOCH₂ Ph, CH₂ SO₂ CH₂ Ph, CH₂ CH₂ SO₂ CH₂ Ph, CH₂ CHMeSO₂ CH₂ Ph, CH₂ COPh, CH₂ CH₂ COPh, CHMeCOPh, CH₂ COCH₂ Ph, CH₂ CH₂ COCH₂ Ph, CHMeCOCH₂ Ph, CH₂ C (C1)═CH₂, Ph, CH₂ SOPh, CH₂ SO₂ Ph, CH₂ Ph-4-OMe, CH₂ Ph-4-Cl, CH₂ C (br)═CH₂, CH₂ C (Cl)═CHCl, CH₂ CH═C (I) Me, CH₂ CH═CHI, CH₂ C (F)═CHCl, CH₂ CH═CBr₂, CH₂ CH═CHr, CH₂ C (Cl)═CHMe, CH₂ C (F)═CHBr, CH₂ C (Br)═CHCl, CH₂ C (Br)═CCl₂, CH₂ CH═CHCH₂ F, CH₂ C (I)═CH₂, CH₂ C (Br)═C (Cl) Me, CH₂ C (I)═CHMe, CH₂ C (Cl)═CCl₂, CH₂ CH═CHCCl₃, CH₂ C (Br)═CHMe, CH₂ C (Cl)═CHF, CH₂ C (Br)═CHF, CH₂ CH═C (Cl) Br, CH₂ C (F)═C (Cl) CF₃, CH₂ C (Cl)═C (Cl) Me, CH₂ C (Br)═CHBr, CH₂ CH═C (F) CF₂ Cl, CH₂ C (Br) Me, CH₂ CH═C (F) CF₃, CH₂ CH═CCl₁, CH₂ C (F)═CH₂, CH₂ CH═CHCCl₃, CH₂ CH═C (F) Cl, CH₂ C (Cl)═C (F) Cl, CH₂ C (F)═CCl₂, CH₂ C (Cl)═CF₂, CH₂ C (CF₃)═CH₂, CMe₂ CH═CH₂, CMe₂ C.tbd.CH, CH₂ CH₂ I, CH₂ C.tbd.C-CN, CH₂ NHBu-n, CH₂ HNSO₂ Me, CH₂ NHSO₂ Et, CH₂ CH₂ NHSO₂ Me, CH₂ CH₂ NHSO₂ Et, CH₂ NHCOMe, CH₂ NHCOEt, CH₂ CH₂ NHCOMe, CH₂ CH₂ NHCOEt

Specific examples for the substituents R^(a2) and R^(a3) of the compound of the present invention

H, Me, Et, Pr-n, Pr-iso, Bu-n, Bu-iso, Bu-sec, Bu-tert, CH₂ F, CHF₂, CF₂, CH₂ Cl, CH₂ Br, CH₂ CF₃, CH₂ CH₂ F, CH₂ CH₂ Cl, CH₂ CH₂ Br, CF₂ CF₃, OMe, OEt, OPr-n, OPr-iso, OCF₃, OCH₂ CF₃, SMe, SEt, SPr-n, SPr-iso, SOMe, SOEt, SOPr-n, SOPr-iso, SO₂ Me, SO₂ Et, SO₂ Pr-n, SO₂ Pr-iso, CO₂ Me, CO₂ Et, CO₂ Pr-n, CO₂ Pr-iso, CO₂ Bu-n, COMe, COEt, COPr-n, COPr-iso, COBu-n, F, Cl, Br, I, NO₂, CN, Ph

Specific examples for the substituents R^(a4) and R^(a5) of the compound of the present invention

H, Me, Et, Pr-n, Pr-iso, Bu-n, Bu-iso, Bu-sec, Bu-tert, Pen-n, Hex-n, Hep-n, CH═CH₂, CH═CHMe, CH═CHEt, CMe═CH₂, CH═CMe₂, CMe═CHMe, CMe═CMe₂, CH₂ CH═CH₂, CH₂ CH═CHMe, CHMeCH═CH₂, CHMeCH═CHMe, CMe₂ CH═CH₂, CMe₂ CH═CHMe, C.tbd.CH, C.tbd.CMe, C.tbd.CEt, CH₂ C.tbd.CH, CH₂ C.tbd.CMe, CHMeC.tbd.CH, CHMeC.tbd.CMe, CMe₂ C.tbd.CH, CMe₂ C.tbd.CMe, Ph

Specific examples for the substituent R^(a6) of the compound of the present invention

Me, Et, Pr-n, Pr-iso, Bu-n, Bu-iso, Bu-sec, Bu-tert, Pen-n, Hex-n, Hep-n, CH₂ CH═CH₂, CH₂ CH═CHMe, CH₂ CH═CHEt, CH₂ CH₂ CH═CH₂, CH₂ CH₂ CH═CHMe, CH₂ CH═CMe₂, CHMeCH═CH₂, CH₂ CMe═CH₂, CH₂ CMe═CHMe, CHMeCH═CHMe, CH₂ CMe═CHEt, CH₂ CH₂ CH═CHMe₂, CH₂ CMe═CMe₂, CMe₂ CH═CH₂, CMe₂ CH═CHMe, CH₂ C.tbd.CH, CH₂ C.tbd.CMe, CH₂ C.tbd.CEt, CH₂ CH₂ C.tbd.CH, CH₂ CH₂ C.tbd.CMe, CHMeC.tbd.CH, CHMeC.tbd.CMe, CMe₂ C.tbd.CH, CMe₂ C.tbd.CMe Ph

Specific examples for the substituent R^(b2) of the compound of the present invention

H, Me, Et, Pr-n, Pr-iso, Bu-n, Bu-iso, Bu-sec, Bu-tert, CH₂ F, CHF₂, CF₃, CH₂ Cl, CH₂ Br, CH₂ CF₂, CH₂ CH₂ F, CH₂ CH₂ Cl, CH₂ CH₂ Br, CF₂ CF₂, OMe, OEt, OPr-n, OPr-iso, OCF₃, OCH₂ CF₃, SMe, Set, SPr-n, Spr-iso, SOMe, SOEt SOPr-n, SOPr-iso, SO₂ Me, SO₂ Et, SO₂ Pr-n, SO₂ Pr-iso, CO₂ Me, CO₂ Et, CO₂ Pr-n, CO₂ Pr-iso, CO₂ Bu-n, COMe, COEt, COPr-n, COPr-iso, COBu-n, F, Cl, Br, I, NO₂, CN, Ph

Specific examples for the substituent R^(b3) of the compound of the present invention

Me, Et, Pr-n, Pr-iso, Bu-n, Bu-iso, Bu-sec, Bu-tert, Pen-n, Hex-n, CH₂ CH═CH₂, CH₂ CH═CHMe, CH₂ CH═CHEt, CH₂ CH₂ CH═CH₂, CH₂ CH₂ CH═CHMe, CH₂ CH═CMe₂, CHMeCH═CH₂, CH₂ CMe═CH₂, CH₂ CMe═CHMe, CHMeCH═CHMe, CH₂ CMe═CHEt, CH₂ CH₂ CH═CMe₂, CH₂ CMe═CMe₂, CH₂ C.tbd.CH, CH₂ C.tbd.CMe, CH₂ C.tbd.CEt, CH₂ CH₂ C.tbd.CH, CH₂ CH₂ C.tbd.CMe, CHMeC.tbd.CH, CHMeC.tbd.CMe

Specific examples for the substituent R^(b4) of the compound of the present invention

H, Me, Et, Pr-n, Pr-iso, Bu-n, Pen-n, Hex-n

Specific examples for the substituent R^(b5) of the compound of the present invention

H, Me, Et, Pr-n, Pr-iso, Bu-n, Pen-n, Hex-n

Specific examples for the substituent R^(cl) of the compound of the present invention

Me, Et, Pr-n, Pr-iso, Bu-n, Bu-iso, Bu-sec, Bu-tert, Pen-n, Hex-n, Hep-n, Pr-cyc, Bu-cyc, Pen-cyc, Hex-cyc, CH₂ Pr-cyc, CH₂ CH₂ Pr-cyc, CHMe-Pr-cyc, CH₂ CHMe-Pr-cyc, CHMe CH₂ Pr-cyc, CH₂ Bu-cyc, CH₂ CH₂ Bu-cyc, CH₂ Pen-cyc, CH₂ Hex-cyc, ##STR7## CH₂ CH═CH₂, CH₂ CH═CHMe, CH₂ CH═CHEt, CH₂ CH₂ CH═CH₂, CH₂ CH₂ CH═CHMe, CH₂ CH═CHMe₂, CHMeCH═CH₂, CH₂ CMe═CH₂, CH₂ CMe═CHMe, CHMeCH═CHMe, CH₂ CMe═CHEt, CH₂ CH₂ CH═CMe₂, CH₂ CMe═CMe₂, CH₂ C.tbd.CH, CH₂ C.tbd.CMe, CH₂ C.tbd.CEt, CH₂ CH₂ C.tbd.CH, CH₂ CH₂ C.tbd.CMe, CHMeC.tbd.CH, CHMeC.tbd.CMe, CH₂ OMe, CH₂ OEt, CH₂ OPr-n, CH₂ OPr-iso, CH₂ CH₂ OMe, CH₂ CH₂ OEt, CH₂ CH₂ OPr-n, CHMeOMe, CHMeOEt, CH₂ CHMeOMe, CH₂ CHMeOEt, CH₂ CH₂ CH₂ OMe, CH₂ CH₂ CH₂ OEt, CH₂ OCH₂ CH═CH₂, CH₂ OCH₂ CH═CHMe, CH₂ CH₂ OCH₂ CH═CH₂, CH₂ CH₂ OCH₂ CH═CHMe, CH₂ OCH₂ C.tbd.CH, CH₂ OCH₂ C.tbd.CMe, CH₂ OCHMeC.tbd.CH, CH₂ OCMe₂ C.tbd.CH, CH₂ CH₂ OCH₂ C.tbd.CH, CH₂ CH₂ OCH₂ C.tbd.CMe, CH₂ CH₂ OCHMeC.tbd.CH, CH₂ CH₂ OCMe₂ C.tbd.CH, CH₂ OCHF₂, CH₂ OCF₃, CH₂ ODF₂ CF₃, CH₂ CH₂ OCHF₂, CH₂ CH₂ OCF₃, CH₂ CH₂ OCF₂ CF₃, CH₂ OCH₂ CF₃, CH₂ CH₂ OCH₂ CF₃, CH₂ OCH₂ CHF₂, CH₂ CH₂ OCH₂ CHF₂, CH₂ OCH₂ CH₂ F, CH₂ OCH₂ CH₂ Cl, CH₂ OCH₂ CH₂ Br, CH₂ CH₂ OCH₂ CH₂ F, CH₂ CH₂ OCH₂ CH₂ Cl, CH₂ CH₂ OCH₂ CH₂ Br, CH₂ OCH₂ CH═CHCl, CH₂ CH₂ OCH₂ CH═CHCl, CH₂ OCH₂ CH═CHBr, CH₂ CH₂ OCH₂ CH═CHBr, CH₂ OCH₂ CF═CF₂, CH₂ CH₂ OCH₂ CF═CF₂, CH₂ OCH═CHCl, CH₂ CH₂ OCH═CHCl, CH₂ OCF═CF₂, CH₂ CH₂ OCF═C₂, CH₂ OCF₂ CF═CF₂, CH₂ CH₂ OCF₂ CF═CF₂, CH₂ OCH₂ CH═CF₂, CH₂ CH₂ OCH₂ CH═CH₂, CH₂ OCH₂ CH═CHCF₃, CH₂ CH₂ OCH₂ CH═CHCF₃, CH₂ OCH₂ C.tbd.CI, CH₂ OCH₂ CH₂ C.tbd.CI, CH₂ CH₂ OCH₂ C.tbd.CI, CH₂ OCH₂ C.tbd.CCF₃, CH₂ CH₂ OCH₂ C.tbd.CCF₃, CH₂ OCMe₂ C.tbd.CI, CH₂ CH₂ OCMe₂ C.tbd.CI, CH₂ OCMe₂ C.tbd.CCF₃, CH₂ CH₂ OCMe₂ C.tbd.CCF₃, CH₂ SMe, CH₂ SEt, CH₂ SPr-n, CH₂ CH₂ SMe, CH₂ CH₂ SEt, CH₂ CH₂ SPr-n, CHMeSMe, CHMeSEt, CH₂ CHMeSMe, CH₂ CHMeSEt, CH₂ SOMe, CH₂ SOEt, CH₂ SOPr-n, CH₂ CH₂ SOMe, CH₂ CH₂ SOEt, CH₂ CH₂ SOPr-n, CHMeSOMe, CHMeSOEt, CH₂ CHMeSOMe, CH₂ CHMeSOEt, CH₂ SO₂ Me, CH₂ SO₂ Et, CH₂ SO₂ Pr-n, CH₂ CH₂ SO₂ Me, CH₂ CH₂ SO₂ Et, CH₂ CH₂ SO₂ Pr-n, CHMeSO₂ Me, CHMeSO₂ Et, CH₂ CHMeSO₂ CHMeSO₂ Et, CH₂ CH₂ F, CH₂ CHF₂, CH₂ CF₃, CH₂ CH₂ Cl, CH₂ CH₂ Br, CH₂ CCl₃, CH₂ CH₂ CF₃, CH₂ CH₂ CCl₃, CH₂ CH₂ CH₂ F, CH₂ CH₂ CH₂ Cl, Cf₂ CF₃, CH₂ CF₂ CF₃, CH₂ CH═CHCl, CH₂ CH═CHBr, CH₂ CH═CF₂, CH₂ CF═CF₂, CH₂ CH═CHCF₃, CH₂ CH═CBrMe, CH═CClMe, CH₂ CH═C (CF₃) Me, CF₂ CF═CF₂, CH₂ C.tbd.CI, CH₂ CH₂ C.tbd.CI, CH₂ C.tbd.CCF₃ CH₂ CH₂ C.tbd.CCF₃, CH₂ CN, CH₂, CH₂, CN, CHMe CN, CH₂ CHMeCN, CH₂ CMe₂ CN, CH₂ CH═CHCN, CH₂ CH(CN) CH═CH₂, CH₂ C (CN)═CH₂, CH₂ C (CN)═CHMe, CH₂ CH (CN) C.tbd.CN, CH₂ CH (CN) C.tbd.C-Me, CH (CN) C.tbd.CH, CH₂ NO₂, CH₂ CH₂ NO₂, CH₂ CHMeNO₂, CH₂ CMe₂ NO₂, CH₂ CH₂ CH₂ NO₂, CH₂ CH═CHNO₂, CH₂ CH (NO₂) CH═CH₂, CH₂ C (NO₂)═CH₂, CH₂ C(NO₂)═CHMe, CH₂ CH (NO₂) C═CH, CH₂ CH (NO₂) C.tbd.CMe, CH₂ CO₂ Me, CH₂ CO₂ Et, CH₂ CO₂ Pr-n, CH₂ CO₂ Pr-iso, CH₂ CO₂ Bu-n, CHMeCO₂ Me, CHMeCO₂ Et, CH₂ CH₂ CO₂ Me, CH₂ CH₂ CO₂ Et, CH₂ CHMeCO₂ Me, CH₂ CH₂ CH₂ CO₂ Me, CH₂ CH═CHCO₂ Me, CH₂ CH═CHCO₂ Et, CH₂ CH═CHCO₂ Pr-n, CH₂ CH═CMeCO₂ Me, CH₂ CMe═CHCO₂ Me, CHMeCH═CHCO₂ Me, CHMeCH═CHCO₂ Et, CH₂ CH₂ CH═CHCO₂ Me, CH₂ CH═CHCH₂ CO₂ Me, CH₂ C.tbd.CC)₂ Me, CH₂ C.tbd.CCO₂ Et, CH₂ C.tbd.CCO₂ Pr-n, CH₂ CH₂ C.tbd.CCO₂ Me, CH₂ CHMeC.tbd.CCO₂ Me, CH₂ CMe₂ C.tbd.CCO₂ Me, CH₂ C.tbd.CCH₂ CO₂ Me, CH₂ COMe, CH₂ COEt, CH₂ COPr-n, CH₂ CH₂ COMe, CH₂ CH₂ COEt, CH₂ CHMeCOMe, CH₂ CMe₂ COMe, CH₂ COCF₃, CH₂ COCCl₃, CH₂ CH₂ COCF₃, CH₂ COCH₂ CF₃, CH₂ COCH₂ CHF₂, CH₂ COCH₂ CHCl₂, CH₂ COCH₂ F, CH₂ COCH₂ Cl, CH₂ COCH₂ Br, CH₂ COCH═CH₂, CH₂ COCH═CHMe, CH₂ COCH₂ CH═CH₂, CH₂ CH₂ COCH═CH₂, CH₂ CH₂ COCH═CHMe, CH₂ COC.tbd.CH, CH₂ COC.tbd.CMe, CH₂ COCH₂ C.tbd.CH, CH₂ CH₂ COC.tbd.CH, CH₂ CH₂ COC.tbd.CMe, CH₂ COCH₂ OMe, CH₂ COCH₂ OEt, CH₂ COCH₂ CH₂ OMe, CH₂ COCH₂ CH₂ OEt, CH₂ CH₂ COCH₂ OMe, CH₂ CH₂ COCH₂ OEt, CH₂ COCH₂ SMe, CH₂ COCH₂ SEt, CH₂ COCH₂ CH₂ SMe, CH₂ COCH₂ CH₂ SEt, CH₂ CH₂ COCH₂ SMe, CH₂ CH₂ COCH₂ SEt, CH₂ COCH₂ SOMe, CH₂ COCH₂ SOEt, CH₂ COCH₂ CH₂ SOMe, CH₂ COCH₂ CH₂ SOEt, CH₂ CH₂ COCH₂ SOMe, CH₂ CH₂ COCH₂ SOEt, CH₂ COCH₂ SO₂ Me, CH₂ COCH₂ SO₂ Et, CH₂ COCH₂ CH₂ SO₂ Me, CH₂ COCH₂ CH₂ SO₂ Et, CH₂ CH₂ COCH₂ SO₂ Me, CH₂ CH₂ COCH₂ SO₂ Et, CH₂ CH═CHCOMe, CH₂ CH═CHCOEt, CHMeCH═CHCOMe, CHMeCH═CHCOEt, CH₂ C.tbd.CCOMe, CH₂ C.tbd.CCOEt, CHMeC.tbd.CCOMe, CHMeC.tbd.CCOEt, CH₂ SO₂ NHMe, CH₂ SO₂ NHEt, CH₂ SO₂ NJPr-n, CH₂ CH₂ SO₂ NHMe, CH₂ CH₂ SO₂ NHEt, CH₂ CH₂ SO₂ NHPr-n, CH₂ SO₂ NHOMe, CH₂ SO₂ NHOEt, CH₂ SO₂ NJOPr-n, CH₂ CH₂ SO₂ NHOMe, CH₂ CH₂ SO₂ NHOEt, CH₂ CH₂ SO₂ NHOPr-n, CH₂ SO₂ NMe₂, CH₂ SO₂ NMeEt, CH₂ SO₂ NEt₂, CH₂ CH₂ SO₂ NMe₂, CH₂ CH₂ SO₂ NMeEt, CH₂ CH₂ SO₂ NEt₂, CH₂ SO₂ N (OMe) Me, CH₂ SO₂ N (OMe) Et, CH₂ SO₂ N (OEt) Me, CH₂ CH₂ SO₂ N (OMe) Me, CH₂ CH₂ SO₂ N (OMe) Et, CH₂ CH₂ SO₂ N (OEt) Me, CH₂ SO₂ N (OEt) Et, CH₂ CH₂ SO₂ N (OEt) Et, CH₂ CONHMe, CH₂ CONHEt, CH₂ CONHPr-n, CH₂ CH₂ CONHMe, CH₂ CH₂ CONHEt, CH₂ CH₂ CONHPr-n, CH₂ CONMe₂, CH₂ CONMe Et, CH₂ CONEt₂, CH₂ CH₂ CONMe₂, CH₂ CH₂ CONMeEt, CH₂ CH₂ CONEt₂, CH₂ CONHOMe, CH₂ CONHOEt, CH₂ CONHOPr-n, CH₂ CH₂ CONHOMe, CH₂ CH₂ CONHOEt, CH₂ CH₂ CONHOPr-n, CH₂ CON (OMe) Me, CH₂ CON (OMe) Et, CH₂ CON (OEt) Me, CH₂ CH₂ CON (OMe) Me, CH₂ CH₂ CON (OMe) Et, CH₂ CH₂ CON (OEt) Me, CH₂ CON (OEt) Et, CH₂ CH₂ CON (OEt) Et, CH₂ NHMe, CH₂ NHEt, CH₂ NHPr-n, CH₂ CH₂ NHMe, CH₂ CH₂ NHEt, CH₂ CH₂ NHPr-n, CH₂ CHMeNHMe, CH₂ CHMeNHEt, CH₂ CHMeNHPr-n, CH₂ CH₂ CH₂ NHMe, CH₂ NHOMe, CH₂ NHOEt, CH₂ NHOPr-n, CH₂ CH₂ NHOMe, CH₂ CH₂ NHOEt, CH₂ CH₂ NHOPr-n, CH₂ CHMeNHOMe, CH₂ CHMeNHOEt, CH₂ CHMeNHOPr-n, CH₂ NMe₂, CH₂ NMeEt, CH₂ NMePr-n, CH₂ CH₂ NMe₂, CH₂ CH₂ NMeEt, CH₂ CH₂ NMePr-n, CH₂ NEt₂, CH₂ CH₂ NEt₂, CH₂ N (OMe) Me, CH₂ N (OMe) Et, CH₂ N (OEt) Me, CH₂ N (OEt) Et, CH₂ CH₂ N (OMe) Me, CH₂ CH₂ N (OMe) Et, CH₂ CH₂ N (OEt) Me, CH₂ CH₂ N (OEt) Et, CH₂ NMeCOMe, CH₂ NEtCOMe, CH₂ NMeCOEt, CH₂ CH₂ NMeCOMe, CH₂ CH₂ NEtCOMe, CH₂ CH₂ NMeCOEt, CH₂ N (OMe) COMe, CH₂ N (OEtCOMe, CH₂ N(OMe) COEt, CH₂ CH₂ N (OMe) COMe, CH₂ CH₂ N (OEt) COMe, CH₂ CH₂ N (OMe) COEt, CH₂ NMe SO₂ Me, CH₂ NEtSO₂ Me, CH₂ NMeSO₂ Et, CH₂ CH₂ NMeSO₂ Me, CH₂ CH₂ NEtSO₂ Me, CH₂ CH₂ NMeSO₂ Et, CH₂ N (OMe) SO₂ Me, CH₂ N (OEt) SO₂ Me, CH₂ N (OMe) SO₂ Et, CH₂ CH₂ N (OMe) SO₂ Me, CH₂ CH₂ N (OEt) SO₂ Me, CH₂ CH₂ N (OMe) SO₂ Et, CH₂ Ph, CH₂ CH₂ Ph, CH₂ CH₂ CH₂ Ph, CHMePh, CH₂ CHMePh, CH₂ CMe₂ Ph, CH₂ CH═CHPh, CH₂ CH═CMePh, CHMeCH═CHPh, CH₂ CMe═CMePh, CHMeCMe═CMePh, CH₂ C.tbd.CPh, CHMeC.tbd.CPh, CH₂ CMe₂ C.tbd.CPh, CH₂ CH₂ OPh, CH₂ CHMeOPh, CH₂ CMe₂ OPh, CH₂ OPh, CH₂ CH₂ SPh, CH₂ CHMeSPh, CH₂ CMe₂ SPh, CH₂ SPh, CH₂ CH₂ SOPh, CH₂ CHMeSOPh, CH₂ CMe₂ SOPh, CH₂ CH₂ SO₂ Ph, CH₂ CHMeSO₂ Ph, CH₂ CMe₂ SO₂ Ph, CH₂ OCH₂ Ph, CH₂ CH₂ OCH₂ Ph, CH₂ CHMe OCH₂ Ph, CH₂ SCH₂ Ph, CH₂ CH₂ SCH₂ Ph, CH₂ CHMe SCH₂ Ph, CH₂ SOCH₂ Ph, CH₂ CH₂ SOCH₂ Ph, CH₂ CHMeSOCH₂ Ph, CH₂ SO₂ CH₂ Ph, CH₂ CH₂ SO₂ CH₂ Ph, CH₂ CHMeSO₂ CH₂ Ph, CH₂ COPh, CH₂ CH₂ COPh, CHMeCOPh, CH₂ COCH₂ Ph, CH₂ CH₂ COCH₂ Ph, CHMeCOCH₂ Ph, CH₂ C (Cl)═CH₂, Ph, CH₂ SOPh, CH₂ SO₂ Ph, CH₂ C (Cl)═CHCl. CH₂ CH═C (I) Me, CH₂ CH═CHI, CH₂ C (F)═CHCl, CH₂ CH═CBr₂, CH₂ CH═CHF, CH₂ C(Cl)═CHMe, CH₂ C (F)═CHBr, CH₂ C (Br)═CHCl, CH₂ C (Br)═CCl₂, CH₂ CH═CHCH₂ F, CH₂ C (Br)═CH₂, CH₂ C (I)═CH₂, CH₂ C (Br)═C (Cl) Me, CH₂ C (I)═CHMe, CH₂ C(Cl)═CCl₂, CH₂ CH═CHCCl₃, CH₂ C (Br)═CHMe, CH₂ C (Cl)═CHF, CH₂ C (Br)═CHF, CH₂ CH═C (Cl) Br, CH₂ C (F)═C (Cl) CF₃, CH₂ C (Cl)═C (Cl) Me, CH₂ C (Br)═CHBr, CH₂ CH═C (F) CF₂ Cl, CH₂ C (Br)═C (Br) Me, CH₂ CH═C (F) CF₃, CH₂ CH═CCl₂, CH₂ C (F)═CH₂, CH₂ CH═CHCCl₃, CH₂ CH═C (F) Cl, CH₂ C (Cl)═C (F) Cl, CH₂ C (F)═CCl₂, CH₂ C (Cl)═CF₂, CH₂ C (CF₃)═CH₂, CMe₂ CH═CH₂, CMe₂ C.tbd.CH, CH₂ CH₂ I, CH₂ C.tbd.C-CN, CH₂ NHBu-n, CH₂ NHSO₂ Me, CH₂ NHSO₂ Et, CH₂ CH₂ NHSO₂ Me, CH₂ CH₂ NHSO₂ Et, CH₂ NHCOMe, CH₂ NHCOEt, CH₂ CH₂ NHCOMe, CH₂ CH₂ NHCOEt

Specific examples for the substituents R^(c2), R^(c3), R^(c4), R^(c5), R^(c6), R^(c11), and R^(c12) of the compound of the present invention

H, Me, Et, Pr-n, Pr-iso, Bu-n, Bu-iso, Bu-sec, Bu-tert, Pen-n Hex-n, Hep-n, CH═CH₂, CH═CHMe, CMe═CH₂, CH═CMe₂, CH═CHEt, CMe═CHMe, CMe═CMe₂, CH₂ CH═CH₂, CH₂ CH═CHMe, CHMeCH═CH₂, CMe₂ CH═CH₂, C.tbd.CH, C.tbd.CMe, C.tbd.CEt, CH₂ C.tbd.CH, CHMeC.tbd.CH, CMe₂ C.tbd.CH, Ph

Specific examples for the substituents R^(c7), R^(c8), R^(c9), R^(c10), R^(c13), and R^(c14) of the compound of the present invention

H, Me, Et, Pr-n, Pr-iso, Bu-n, Bu-iso, Bu-sec, Bu-tert, Pen-n, Hex-n, CH₂ F, CHF₂, CF₃, CH₂ Cl, CH₂ Br, CH₂ CF₃, CH₂ CH₂ F, CH₂ CH₂ Cl, CH₂ CH₂ Br, CF₂ CF₃, OMe, OEt, OPr-n, OPr-iso, OCF₃, OCH₂ CF₃, SMe, SEt, SPr-n, SPr-iso, SOMe, SOEt, SOPr-n, SOPr-iso, SO₂ Me, SO₂ Et, SO₂ Pr-n, SO₂ Pr-iso, CO₂ Me, CO₂ Et, CO₂ Pr-n, CO₂ Pr-iso, CO₂ Bu-n, COMe, COEt, COPr-n, COPr-iso, COBu-n, F, Cl, Br, I, NO₂, CN, Ph

Specific examples for the substituents R^(d2), R^(d3) and R^(d4) of the compound of the present invention

H, Me, Et, Pr-n, Pr-iso, Bu-n, Bu-iso, Bu-sec, Bu-tert, Pen-n, Hex-n, Hep-n, CH═CH₂, CH═CHMe, CH═CHEt, CMe═CH₂, CH═CMe₂, CMe═CHMe, CMe═CMe₂, CH₂ CH═CH₂, CH₂ CH═CHMe, CHMeCH═CH₂, CHMeCH═CHMe, CMe₂ CH═CH₂, CMe₂ CH═CHMe, CH.tbd.CH, C.tbd.CMe, C.tbd.CEt, CH₂ C.tbd.CH, CH₂ C.tbd.CMe, CHMeC.tbd.CH, CHMeC.tbd.CMe, CMe₂ C.tbd.CH, CMe₂ C.tbd.CMe, Ph

Specific examples for the substituent R^(d5) of the compound of the present invention

Me, Et, Pr-n, Pr-iso, Bu-n, Bu-iso, Bu-sec, Bu-tert, Pen-n, Hex-n, Hep-n, CH₂ CH═CH₂, CH₂ CH═CHMe, CH₂ CH═CHEt, CH₂ CH₂ CH═CH₂, CH₂ CH₂ CH═CHMe, CH₂ CH═CMe₂, CHMeCH═CH₂, CH₂ CMe═CH₂, CH₂ CMe═CHMe, CHMeCH═CHMe, CH₂ CMe═CHEt, CH₂ CH₂ CH═CMe₂, CH₂ CMe═CMe₂, CMe₂ CH═CH₂, CMe₂ CH═CHMe, CH₂ C.tbd.CH, CH₂ C.tbd.CMe, CH₂ C.tbd.CEt, CH₂ CH₂ C.tbd.CH, CH₂ CH₂ C.tbd.CMe, CHMeC.tbd.CH, CHMeC.tbd.CMe, CMe₂ C.tbd.CH, CMe₂ C.tbd.CMe, Ph

Specific examples for the substituents R^(d6) and R^(f2) of the compound of the present invention

Me, Et, Pr-n, Pr-iso, Bu-n, Bu-iso, Bu-sec, Bu-tert, Pen-n, Hex-n, Hep-n, CH₂ CH═CH₂, CH₂ CH═CHMe, CH₂ CH═CHEt, CH₂ CH₂ CH═CH₂, CH₂ CH₂ CH═CHMe, CH₂ CH═CMe₂, CHMeCH═CH₂, CH₂ CMe═CH₂, CH₂ CMe═CHMe, CHMeCH═CHMe, CH₂ CMe═CHEt, CH₂ CH₂ CH═CMe₂, CH₂ CMe═CMe₂, CMe₂ CH═CH₂, CMe₂ CH═CHMe, CH₂ C.tbd.CH, CH₂ C.tbd.CMe, CH₂ C.tbd.CEt, CH₂ CH₂ C.tbd.CH, CH₂ CH₂ C.tbd.CMe, CHMeC.tbd.CH, CHMeC.tbd.CMe, CMe₂ C.tbd.CH, CMe₂ C.tbd.CMe, CH₂ SMe, CH₂ SEt, CH₂ SPr-n, CH₂ SBu-n, CH₂ CH₂ SMe, CH₂ CH₂ SEt, CH₂ CH₂ SPr-n, CH₂ SOMe, CH₂ SOEt, CH₂ SOPr-n, CH₂ CH₂ SOMe, CH₂ CH₂ SOEt, CH₂ CH₂ SOPr-n, CH₂ SO₂ Me, CH₂ SO₂ Et, CH₂ SO₂ Pr-n, CH₂ SO₂ Bu-n, CH₂ CH₂ SO₂ Me, CH₂ CH₂ SO₂ Et, CH₂ CH₂ SO₂ Pr-n, CH₂ OMe, CH₂ OEt, CH₂ OPr-n, CH₂ OBu-n, CH₂ CH₂ OMe, CH₂ CH₂ OEt, CH₂ CH₂ OPr-n, CH₂ CO₂ Me, CH₂ CO₂ Et, CH₂ CO₂ Pr-n, CH₂ CO₂ Bu-n, CHMeCO₂ Me, CHMeCO₂ Et, CHMeCO₂ Pr-n, CMe₂ CO₂ Me, CMe₂ CO₂ Et, CH₂ COMe, CH₂ COEt, CH₂ COPr-n, CH₂ COBu-n, CH₂ CH₂ COMe, CH₂ CH₂ COEt, CH₂ CH₂ COPr-n, CH₂ CN, CH₂ CH₂ CN, CH₂ CH₂ CH₂ CN, Ph, CH₂ Ph, CH₂ CH₂ PH, CHMePh

Specific examples for the substituents R^(e2), R^(e3), R^(e6) and R^(e7) of the compound of the present invention

H, Me, Et, Pr-n, Pr-iso, Bu-n, Bu-iso, Bu-sec, Bu-tert, Pen-n, Hex-n, CH₂ F, CHF₂, CF₃, CH₂ Cl, CH₂ Br, CH₂ CF₃, CH₂ CH₂ F, CH₂ CH₂ Cl, CH₂ CH₂ Br, CF₂ CF₃, OMe, OEt, OPr-n, OPr-iso, OCF₃, OCH₂ CF₃, SMe, SEt, SPr-n, SPr-iso, SOMe, SOEt, SOPr-n, SOPr-iso, SO₂ Me, SO₂ Et, SO₂ Pr-n, SO₂ Pr-iso, CO₂ Me, CO₂ Et, CO₂ Pr-n, CO₂ Pr-iso, CO₂ Bu-n, COMe, COEt, COPr-n, COPr-iso, COBu-n, F, Cl, Br, I, NO₂, C, Ph

Specific examples for the substituents R^(e4), R^(e5), R^(e8), R^(e9) and R^(e10) of the compound of the present invention

H, Me, Et, Pr-n, Pr-iso, Bu-n, Bu-iso, Bu-sec, Bu-tert, Pen-n, Hex-n, CH═CH₂, CH═CHMe, CH═CHEt, CMe═CH₂, CH═CMe₂, CMe═CHMe, CMe═CMe₂, CH₂ CH═CH₂, CH₂ CH═CHMe, CHMeCH═CH₂, CHMeCH═CHMe, CMe₂ CH═CH₂, CMe₂ CH═CHMe, C.tbd.CH, C.tbd.CMe, C.tbd.CEt, CH₂ C.tbd.CH, CH₂ C.tbd.CMe, CHMeC.tbd.CH, CHMeC.tbd.CMe, CMe₂ C.tbd.CH, CMe₂ C.tbd.CMe, Ph

Specific examples for the substituents R^(f3), R^(f4), R^(f7), R^(f8), R^(f11) and R^(f12) of the compound of the present invention

H, Me, Et, Pr-n, Pr-iso, Bu-n, Bu-iso, Bu-sec, Bu-tert, CH₂ F, CHF₂, CF₃, CH₂ Cl, CH₂ Br, CH₂ CF₃, CH₂ CH₂ F, CH₂ CH₂ Cl, CH₂ CH₂ Br, CF₂ CF₃, OMe, OEt, OPr-n, OPr-iso, OCF₃, OCH₂ CF₃, SMe, SEt, SPr-n, SPr-iso, SOMe, SOEt, SOPr-n, SOPr-iso, SO₂ Me, SO₂ Et, SO₂ Pr-n, SO₂ Pr-iso, CO₂ Me, CO₂ Et, CO₂ Pr-n, CO₂ Pr-iso, CO₂ Bu-n, COMe, COEt, COPr-n, COPr-iso, COBu-n, F, Cl, Br, I, NO₂, CN, Ph

Specific examples for the substituents R^(f5), R^(f6), R^(f9), R^(f10), R^(f13), R^(f14) and R^(f15) of the component of the present invention

H, Me, Et, Pr-n, Pr-iso, Bu-n, Bu-iso, Bu-sec, Bu-tert, Pen-n, Hex-n, Hep-n, CH═CH₂, CH═CHMe, CH═CHEt, CMe═CH₂, CH═CMe₂, CMe═CHMe, CMe═CMe₂, CH₂ CH═CH₂, CH₂ CH═CHMe, CHMeCH═CH₂, CHMeCH═CHMe, CMe₂ CH═CH₂, CMe₂ CH═CHMe, C.tbd.CH, C.tbd.CMe, C.tbd.CEt, CH₂ C.tbd.CH, CH₂ C.tbd.CMe, CHMeC.tbd.CH, CHMeC.tbd.CMe, CMe₂ C.tbd.CH, CMe₂ C.tbd.CMe, Ph

Specific examples for the substituent R^(g1) of the compound of the present invention

Me, Et, Pr-n, Pr-iso, Bu-n, Bu-iso, Bu-sec, Bu-tert, Pen-n, Hex-n, Hep-n, Pr-cyc, Bu-cyc, Pen-cyc, Hex-cyc, CH₂ Pr-cyc, CH₂ CH₂ Pr-cyc, Hex-cyc, CH₂ CHMe-Pr-cyc, CHMeCH₂ Pr-cyc, CH₂ Bu-cyc, CH₂ CH₂ Bu-cyc, CH₂ Pen-cyc, CH₂ Hex-cyc, ##STR8## CH₂ CH═CH₂, CH₂ CH═CHMe, CH₂ CH═CHEt, CH₂ CH₂ CH═CH₂, CH₂ CH₂ CH═CHMe, CH₂ CH═CMe₂, CHMeCH═CH₂, CH₂ CMe═CH₂, CH₂ CMe═CHMe, CHMeCH═CHMe, CH₂ CMe═CHEt, CH₂ CH₂ CH═CMe₂, CH₂ CMe═CMe₂, CH₂ .tbd.CH, CH₂ C.tbd.CMe, CH₂ C.tbd.CEt, CH₂ CH₂ C.tbd.CH, CH₂ CH₂ C.tbd.CMe, CHMeC.tbd.CH, CHMeC.tbd.CMe, CH₂ OMe, CH₂ OEt, CH₂ OPr-n, CH₂ OPr-iso, CH₂ CH₂ OMe, CH₂ CH₂ OEt, CH₂ CH₂ OPr-n, CHMeOMe, CHMeOEt, CH₂ CHMeOMe, CH₂ CHMeOEt, CH₂ CH₂ CH₂ OMe, CH₂ CH₂ CH₂ OEt, CH₂ OCH₂ CH═CH₂, CH₂ OCH₂ CH═CHMe, CH₂ CH₂ OCH₂ CH═CH₂, CH₂ CH₂ OCH₂ CH═CHMe, CH₂ OCH₂ C.tbd.CH, CH₂ OCH₂ C.tbd.CMe, CH₂ OCHMeC.tbd.CH, CH₂ OCMe₂ C.tbd.CH, CH₂ CH₂ OCH₂ C.tbd.CH, CH₂ CH₂ OCH₂ C.tbd.CMe, CH₂ CH₂ OCHMeC.tbd.CH, CH₂ CH₂ OCMe₂ C.tbd.CH, CH₂ OCHF₂, CH₂ OCF₃, CH₂ OCF₂ CF₃, CH₂ CH₂ OCHF₂, CH₂ CH₂ OCF₃, CH₂ CH₂ OCF₂ CF₃, CH₂ OCH₂ CF₃, CH₂ CH₂ OCH₂ CF₃, CH₂ OCH₂ CHF₂, CH₂ CH₂ OCH₂ CHF₂, CH₂ OCH₂ CH₂ F, CH₂ OCH₂ CH₂ Cl, CH₂ OCH₂ CH₂ Br, CH₂ CH₂ OCH₂ CH₂ F, CH₂ CH₂ OCH₂ CH₂ Cl, CH₂ CH₂ OCH₂ CH₂ Br, CH₂ OCH₂ CH═CHCl, CH₂ CH₂ OCH₂ CH═CHCl, CH₂ OCH₂ CH═CHBr, CH₂ CH₂ OCH₂ CH═CHBr, CH₂ OCH₂ CF═CF₂, CH₂ CH₂ OCH₂ CF═CF₂, CH₂ OCH═CHCl, CH₂ CH₂ OCH═CHCl, CH₂ OCF═CF₂, CH₂ CH₂ OCF═CF₂, CH₂ OCF₂ CF═CF₂, CH₂ CH₂ OCF₂ CF═CF₂, CH₂ OCH₂ CH═CF₂, CH₂ CH₂ OCH₂ CH═CF₂, CH₂ OCH₂ CH═CHCF₃, CH₂ CH₂ OCH₂ CH═CHCF₃, CH₂ OCH₂ C.tbd.CI, CH₂ OCH₂ CH₂ .tbd.CI, CH₂ CH₂ OCH₂ C.tbd.CI, CH₂ OCH₂ C.tbd.CCF₃, CH₂ CH₂ OCH₂ C.tbd.CCF₃, CH₂ OCMe₂ C.tbd.CI, CH₂ CH₂ OCMe₂ C.tbd.CI, CH₂ OCMe₂ C.tbd.CCF₃, CH₂ CH₂ OCMe₂ C.tbd.CCF₃, CH₂ SMe, CH₂ SEt, CH₂ SPr-n, CH₂ CH₂ SMe, CH₂ CH₂ SEt, CH₂ CH₂ SPr-n, CHMeSMe, CHMeSEt, CH₂ CHMeSMe, CH₂ CHMeSEt, CH₂ SOMe, CH₂ SOEt, CH₂ SOPr-n, CH₂ CH₂ SOMe, CH₂ CH₂ SOEt, CH₂ CH₂ SOPr-n, CHMeSOMe, CHMeSOEt, CH₂ CHMeSOMe, CH₂ CHMeSOEt, CH₂ SO₂ Me, CH₂ SO₂ Et, CH₂ SO₂ Pr-n, CH₂ CH₂ SO₂ Me, CH₂ CH₂ SO₂ Et, CH₂ CH₂ SO₂ Pr-n, CHMeSO₂ Me, CHMeSO₂ Et, CH₂ CHMeSO₂ Me, CH₂ CHMeSO₂ Et, CH₂ CH₂ F, CH₂ CHF₂, CH₂ CF₃, CH₂ CH₂ Cl, CH₂ CH₂ Br, CH₂ CCl₃, CH₂ CH₂ CF₃, CH₂ CH₂ CCl₃, CH₂ CH₂ CH₂ F, CH₂ CH₂ CH₂ Cl, CF₂ CF₃, CH₂ CF₂ CF₃, CH₂ CH═CHCl, CH₂ CH═CHBr, CH₂ CH═CF₂, CH₂ CF═CF₂, CH₂ CH═CHCF₃, CH₂ CH═CBrMe, CH₂ CH═CClMe, CH₂ CH═C(CF₃)Me, CF₂ CF═CF₂, CH₂ C.tbd.CI, CH₂ CH₂ C.tbd.CI, CH₂ C.tbd.CCF₃, CH₂ CH₂ C.tbd.CCF₃, CH₂ CN, CH₂ CH₂ CN, CHMeCN, CH₂ CHMeCN, CH₂ CMe₂ CN, CH₂ CH═CHCN, CH₂ CH(CN)CH═CH₂, CH₂ C(CN)═CH₂, CH₂ C(CN)═CHMe, CH₂ CH(CN)C.tbd.CH, CH₂ CH(CN)C.tbd.C-Me, CH(CN)C.tbd.CH, CH₂ NO₂, CH₂ CH₂ NO₂, CH₂ CHMeNO₂, CH₂ CMe₂ NO₂, CH₂ CH₂ CH₂ NO₂, CH₂ CH═CHNO₂, CH₂ CH(NO₂)CH═CH₂, CH₂ C(NO₂)═CH₂, CH₂ C(NO₂)═CHMe, CH₂ CH(NO₂)C.tbd.CH, CH₂ CH(NO₂)C.tbd.CMe, CH₂ CO₂ Me, CH₂ CO₂ Et, CH₂ CO₂ Pr-n, CH₂ CO₂ Pr-iso, CH₂ CO₂ Bu-n, CHMeCO₂ Me, CHMeCO₂ Et, CH₂ CH₂ CO₂ Me, CH₂ CH₂ CO₂ Et, CH₂ CHMeCO₂ Me, CH₂ CH₂ CH₂ CO₂ Me, CH₂ CH═CHCO₂ Me, CH₂ CH═CHCO₂ Et, CH₂ CH═CHCO₂ Pr-n, CH₂ CH═CMeCO₂ Me, CH₂ CMe═CHCO₂ Me, CHMeCH═CHCO₂ Me, CHMeCH═CHCO₂ Et, CH₂ CH₂ CH═CHCO₂ Me, CH₂ CH═CHCH₂ CO₂ Me, CH₂ C.tbd.CCO₂ Me, CH₂ C.tbd.CCO₂ Et, CH₂ C.tbd.CCO₂ Pr-n, CH₂ CH₂ C.tbd.CCO₂ Me, CH₂ CHMeC.tbd.CCO₂ Me, CH₂ CMe₂ C.tbd.CCO₂ Me, CH₂ C.tbd.CCH₂ CO₂ Me, CH₂ COMe, CH₂ COEt, CH₂ COPr-n, CH₂ CH₂ COMe, CH₂ CH₂ COEt, CH₂ CHMeCOMe, CH₂ CMe₂ COMe, CH₂ COCF₃, CH₂ COCCl.sub., CH₂ CH₂ COCF₃, CH₂ COCH₂ CF₃, CH₂ COCH₂ CHF₂, CH₂ COCH₂ CHCl₂, CH₂ COCH₂ F, CH₂ COCH₂ Cl, CH₂ COCH₂ Br, CH₂ COCH═CH₂, CH₂ COCH═CHMe, CH₂ COCH₂ CH═CH₂, CH₂ CH₂ COCH═CH₂, CH₂ CH₂ COCH═CHMe, CH₂ COC.tbd.CH, CH₂ COC.tbd.CMe, CH₂ COCH₂ C.tbd.CH, CH₂ CH₂ COC.tbd.CH, CH₂ CH₂ COC.tbd.CMe, CH₂ COCH₂ OMe, CH₂ COCH₂ OEt, CH₂ COCH₂ CH₂ OMe, CH₂ COCH₂ CH₂ OEt, CH₂ CH₂ COCH₂ OMe, CH₂ CH₂ COCH₂ OEt, CH₂ COCH₂ SMe, CH₂ COCH₂ SEt, CH₂ COCH₂ CH₂ SMe, CH₂ COCH₂ CH₂ SEt, CH₂ CH₂ COCH₂ SMe, CH₂ CH₂ COCH₂ SEt, CH₂ COCH₂ SOMe, CH₂ COCH₂ SOEt, CH₂ COCH₂ CH₂ SOMe, CH₂ COCH₂ CH₂ SOEt, CH₂ CH₂ COCH₂ SOMe, CH₂ CH₂ COCH₂ SOEt, CH₂ COCH₂ SO₂ Me, CH₂ COCH₂ SO₂ Et, CH₂ COCH₂ CH₂ SO₂ Me, CH₂ COCH₂ CH₂ SO₂ Et, CH₂ CH₂ COCH₂ SO₂ Me, CH₂ CH₂ COCH₂ SO₂ Et, CH₂ CH═CHCOMe, CH₂ CH═CHCOEt, CHMeCH═CHCOMe, CHMeCH═CHCOEt, CH₂ C.tbd.CCOMe, CH₂ C.tbd.CCOEt, CHMeC.tbd.CCOMe, CHMeC.tbd.CCOEt, CH₂ SO₂ NHMe, CH₂ SO₂ NHEt, CH₂ SO₂ NHPr-n, CH₂ CH₂ SO₂ NHMe, CH₂ CH₂ SO₂ NHEt, CH₂ CH₂ SO₂ NHPr-n, CH₂ SO₂ NHOMe, CH₂ SO₂ NHOEt, CH₂ SO₂ NHOPr-n, CH₂ CH₂ SO₂ NHOMe, CH₂ CH₂ SO₂ NHOEt, CH₂ CH₂ SO₂ NHOPr-n, CH₂ SO₂ NMe₂, CH₂ SO₂ NMeEt, CH₂ SO₂ NEt₂, CH₂ CH₂ SO₂ NMe₂, CH₂ CH₂ SO₂ NMeEt, CH₂ CH₂ SO₂ NEt₂, CH₂ SO₂ N(OMe)Me, CH₂ SO₂ N(OMe)Et, CH₂ SO₂ N(OEt)Me, CH₂ CH₂ SO₂ N(OMe)Me, CH₂ CH₂ SO₂ N(OMe)Et, CH₂ CH₂ SO₂ N(OEt)Me, CH₂ SO₂ N(OEt)Et, CH₂ CH₂ SO₂ N(OEt)Et, CH₂ CONHMe, CH₂ CONHEt, CH₂ CONHPr-n, CH₂ CH₂ CONHMe, CH₂ CH₂ CONHEt, CH₂ CH₂ CONHPr-n, CH₂ CONMe₂, CH₂ CONMeEt, CH₂ CONEt₂, CH₂ CH₂ CONMe₂, CH₂ CH₂ CONMeEt, CH₂ CH₂ CONEt₂, CH₂ CONHOMe, CH₂ CONHOEt, CH₂ CONHOPr-n, CH₂ CH₂ CONHOMe, CH₂ CH₂ CONHOEt, CH₂ CH₂ CONHOPr-n, CH₂ CON(OMe)Me, CH₂ CON(OMe)Et, CH₂ CON(OEt)Me, CH₂ CH₂ CON(OMe)Me, CH₂ CH₂ CON(OMe)Et, CH₂ CH₂ CON(OEt)Me, CH₂ CON(OEt)Et, CH₂ CH₂ CON(OEt)Et, CH₂ NHMe, CH₂ NHEt, CH₂ NHPr-n, CH₂ CH₂ NHMe, CH₂ CH₂ NHEt, CH₂ CH₂ NHPr-n, CH₂ CHMeNHMe, CH₂ CHMeNHEt, CH₂ CHMeNHPr-n, CH₂ CH₂ CH₂ NHMe, CH₂ NHOMe, CH₂ NHOEt, CH₂ NHOPr-n, CH₂ CH₂ NHOMe, CH₂ CH₂ NHOEt, CH₂ CH₂ NHOPr-n, CH₂ CHMeNHOMe, CH₂ CHMeNHOEt, CH₂ CHMeNHOPr-n, CH₂ NMe₂, CH₂ NMeEt, CH₂ NMePr-n, CH₂ CH₂ NMe₂, CH₂ CH₂ NMeEt, CH₂ CH₂ NMePr-n, CH₂ NEt₂, CH₂ CH₂ NEt₂, CH₂ N(OMe)Me, CH₂ N(OMe)Et, CH₂ N(OEt)Me, CH₂ N(OEt)Et, CH₂ CH₂ N(OMe)Me, CH₂ CH₂ N(OMe)Et, CH₂ CH₂ N(OEt)Me, CH₂ CH₂ N(OEt)Et, CH₂ NMeCOMe, CH₂ NEtCOMe, CH₂ NMeCOEt, CH₂ CH₂ NMeCOMe, CH₂ CH₂ NEtCOMe, CH₂ CH₂ NMeCOEt, CH₂ N(OMe)COMe, CH₂ N(OEt)COMe, CH₂ N(OMe)COEt, CH₂ CH₂ N(OMe)COMe, CH₂ CH₂ N(OEt)COMe, CH₂ CH₂ N(OMe)COEt, CH₂ NMeSO₂ Me, CH₂ NEtSO₂ Me, CH₂ NMeSO₂ Et, CH₂ CH₂ NMeSO₂ Me, CH₂ CH₂ NEtSO₂ Me, CH₂ CH₂ NMeSO₂ Et, CH₂ N(OMe)SO₂ Me, CH₂ N(OEt)SO₂ Me, CH₂ N(OMe)SO₂ Et, CH₂ CH₂ N(OMe)SO₂ Me, CH₂ CH₂ N(OEt)SO₂ Me, CH₂ CH₂ N(OMe)SO₂ Et, CH₂ Ph, CH₂ CH₂ Ph, CH₂ CH₂ CH₂ Ph, CHMePh, CHMePh, CH₂ CHMePh, CH₂ CMe₂ Ph, CH₂ CH═CHPh, CH₂ CH═CMePh, CHMeCH═CHPh, CH₂ CMe═CMePh, CHMeCMe═CMePh, CH₂ C.tbd.CPh, CHMeC.tbd.CPh, CH₂ CMe₂ C.tbd.CPh, CH₂ CH₂ OPh, CH₂ CHMeOPh, CH₂ CMe₂ OPh, CH₂ OPh, CH₂ CH₂ SPh, CH₂ CHMeSPh, CH₂ CMe₂ SPh, CH₂ SPh, CH₂ CH₂ SOPh, CH₂ CHMeSOPh, CH₂ CMe₂ SOPh, CH₂ CH₂ SO₂ Ph, CH₂ CHMeSO₂ Ph, CH₂ CMe₂ SO₂ Ph, CH₂ OCH₂ Ph, CH₂ CH₂ OCH₂ Ph, CH₂ CHMeOCH₂ Ph, CH₂ SCH₂ Ph, CH₂ CH₂ SCH₂ Ph, CH₂ CHMeSCH₂ Ph, CH₂ SOCH₂ Ph, CH₂ CH₂ SOCH₂ Ph, CH₂ CHMeSOCH₂ Ph, CH₂ SO₂ CH₂ Ph, CH₂ CH₂ SO₂ CH₂ Ph, CH₂ CHMeSO₂ CH₂ Ph, CH₂ COPh, CH₂ CH₂ COPh, CHMeCOPh, CH₂ COCH₂ Ph, CH₂ CH₂ COCH₂ Ph, CHMeCOCH₂ Ph

Specific examples for the substituents R^(g2) and R^(g3) of the compound of the present invention

Me, Et, Pr-n, Pr-iso, Bu-n, Bu-iso, Bu-sec, Bu-tert, Pen-n, Hex-n, CH₂ CH═CH₂, CH₂ CH═CHMe, CH₂ CH═CHEt, CH₂ CH₂ CH═CH₂, CH₂ CH₂ CH═CHMe, CH₂ CH═CMe₂, CHMeCH═CH₂, CH₂ CMe═CH₂, CH₂ CMe═CHMe, CHMeCH═CHMe, CH₂ CMe═CHEt, CH₂ CH₂ CH═CMe₂, CH₂ CMe═CMe₂, CH₂ C.tbd.CH, CH₂ C.tbd.CMe, CH₂ C.tbd.CEt, CH₂ CH₂ C.tbd.CH, CH₂ CH₂ C.tbd.CMe, CHMeC.tbd.CH, CHMeC.tbd.CMe, CH₂ F, CHF₂, CF₃, CH₂ Cl, CH₂ Br, CH₂ CF₃, CH₂ CH₂ F, CH₂ CH₂ Cl, CH₂ CH₂ Br, CF₂ CF₃, OMe, OEt, OPr-n, OPr-iso, SO₂ Me, SO₂ Et, SO₂ Pr-n, SO₂ Pr-iso, SO₂ NHMe, SO₂ NHEt, SO₂ NHPr-n, SO₂ NHPr-iso, SO₂ NMe₂, SO₂ NEt₂, SO₂ N(Pr-n)₂, SO₂ NMeEt, SO₂ NMePr-n, CO₂ Me, CO₂ Et, CO₂ Pr-n, CO₂ Pr-iso, CO₂ Bu-n, COMe, COEt, COPr-n, COPr-iso, COBu-n, CONHMe, CONHEt, CONHPr-n, CONHPr-iso, CONMe₂, CONEt₂, CON(Pr-n)₂, CONMeEt, CONMePr-n, Ph, PhCH₂

Specific examples of --NR^(g2) R^(g3) wherein the substituents R^(g2) and R^(g3) of the compound of the present invention form a saturated 3- to 7-membered heterocyclic ring together with the nitrogen atom to which they are bonded ##STR9## Specific examples for the substituent L of the compound of the present invention

H, Me, Et, Pr-n, CH₂ CH═CH₂, CH₂ C.tbd.CH

Specific examples for the substituents B and D of the compound of the present invention

Me, Et, Pr-n, OMe, OEt, CH₂ F, CHF₂, CF₃, OCHF₂, OCF₃, F, Cl, Br, NHMe, NHEt, NHPr-n, OCH₂ CF₃, NME₂, OCBrF₂, CH₂ Cl, CH₂ F

Now, examples of the compound covered by the present invention will be presented in the following Tables 1A, 1B, 1C, 2A, 2B, 2C, 3, 4A, 4B, 4C, 5, 6, 7, 8, 9, 10, 11 and 12. However, the compound of the present invention is not limited to such examples. The symbols in these Tables have the following meanings.

Me: methyl group, Et: ethyl group, Pr-n: n-propyl group, Pr-iso: isopropyl group, Bu-n: n-butyl group, Bu-iso: isobutyl group, Bu-sec: sec-butyl group, Bu-tert: tert-butyl group, Pen-n: n-pentyl grup, Hex-n: n-hexyl group, Hep-n: n-heptyl group, Pr-cyc: cyclopropyl group, Bu-cyc: cyclobutyl group, Pen-cyc: cyclopentyl group, Hex-cyc: cyclohexyl group, and Ph: phenyl group, ##STR10## Gn is the same as above G and represents the following Ga, Gb and Gc.

Ga=G1 to G90 (i.e. represents any one of G1 to G90)

Gb=G1 to G13 (i.e. represents any one of G1 to G13)

Gc=G1 to G6 (i.e. represents any one of G1 to G6) ##STR11##

                  TABLE 1A                                                         ______________________________________                                          ##STR12##                                                                                        ##STR13##                                                    ##STR14##                                                                                        ##STR15##                                                    ##STR16##                                                                                        ##STR17##                                                    ##STR18##                                                                                        ##STR19##                                                    ##STR20##                                                                                        ##STR21##                                                    ##STR22##                                                                                        ##STR23##                                                    ##STR24##                                                                                        ##STR25##                                                    ##STR26##                                                                                        ##STR27##                                                    ##STR28##                                                                                        ##STR29##                                                    ##STR30##                                                                                        ##STR31##                                                    ##STR32##                                                                                        ##STR33##                                                    ##STR34##                                                                                        ##STR35##                                                    ##STR36##                                                                                        ##STR37##                                                    ##STR38##                                                                                        ##STR39##                                                    ##STR40##                                                                                        ##STR41##                                                    ##STR42##                                                                                        ##STR43##                                                    ##STR44##                                                                                        ##STR45##                                                    ##STR46##                                                                                        ##STR47##                                                    ##STR48##                                                                                        ##STR49##                                                    ##STR50##                                                                                        ##STR51##                                                    ##STR52##                                                                                        ##STR53##                                                    ##STR54##                                                                                        ##STR55##                                                    ##STR56##                                                                                        ##STR57##                                                    ##STR58##                                                                                        ##STR59##                                                    ##STR60##                                                                                        ##STR61##                                                    ##STR62##                                                                                        ##STR63##                                                    ##STR64##                                                                                        ##STR65##                                                    ##STR66##                                                                                        ##STR67##                                                    ##STR68##                                                                                        ##STR69##                                                    ##STR70##                                                                                        ##STR71##                                                    ##STR72##                                                                                        ##STR73##                                                    ##STR74##                                                                                        ##STR75##                                                    ##STR76##                                                                                        ##STR77##                                                    ##STR78##                                                                                        ##STR79##                                                    ##STR80##                                                                                        ##STR81##                                                    ##STR82##                                                                                        ##STR83##                                                    ##STR84##                                                                                        ##STR85##                                                    ##STR86##                                                                                        ##STR87##                                                    ##STR88##                                                                                        ##STR89##                                                    ##STR90##                                                                                        ##STR91##                                                    ##STR92##                                                                                        ##STR93##                                                    ##STR94##                                                                                        ##STR95##                                                    ##STR96##                                                                                        ##STR97##                                                    ##STR98##                                                                                        ##STR99##                                                    ##STR100##                                                                                       ##STR101##                                                   ##STR102##                                                                                       ##STR103##                                                   ##STR104##                                                                                       ##STR105##                                                   ##STR106##                                                                                       ##STR107##                                                   ##STR108##                                                                                       ##STR109##                                                   ##STR110##                                                                                       ##STR111##                                                   ##STR112##                                                                                       ##STR113##                                                   ##STR114##                                                                    R.sup.m represents R.sup.a1, R.sup.b1, R.sup.d1, R.sup.e1 or R.sup.f1.         R.sup.m                  Gn                                                    ______________________________________                                         Me                       Ga                                                    Et                       Ga                                                    Pr-n                     Ga                                                    Pr-iso                   Ga                                                    Bu-n                     Ga                                                    Bu-iso                   Ga                                                    Bu-sec                   Gb                                                    Bu-tert                  Gb                                                    Pen-n                    Ga                                                    Hex-n                    Gb                                                    Hep-n                    Gb                                                    Pr-cyc                   Ga                                                    Hex-cyc                  Ga                                                    CH.sub.2 Pr-cyc          Ga                                                    CH.sub.2 CH.sub.2 Pr-cyc Ga                                                    CH.sub.2 Bu-cyc          Gb                                                    CH.sub.2 Pen-cyc         Gc                                                    Hexen-cyc                Gb                                                    CH.sub.2 Penten-cyc      Gb                                                    CH.sub.2 CHCH.sub.2      Ga                                                    CH.sub.2 CHCHMe          Ga                                                    CH.sub.2 CHCHEt          Ga                                                    CH.sub.2 CHCMe.sub.2     Gb                                                    CH.sub.2 CMeCH.sub.2     Ga                                                    CH.sub.2 CMeCHCHMe       Gc                                                    CH.sub.2 CH.sub.2 CHCH.sub.2                                                                            Ga                                                    CH.sub.2 CH.sub.2 CHCHMe Gb                                                    CH.sub.2 CCH             Ga                                                    CH.sub.2 CCMe            Ga                                                    CH.sub.2 CCEt            Ga                                                    CH.sub.2 CH.sub.2 CCH    Ga                                                    CH.sub.2 CH.sub.2 CCMe   Gb                                                    CHMeCCH                  Gb                                                    CHMeCCMe                 Gc                                                    CH.sub.2 OMe             Ga                                                    CH.sub.2 OEt             Ga                                                    CH.sub.2 OPr-n           Gb                                                    CH.sub.2 CH.sub.2 OMe    Ga                                                    CH.sub.2 CH.sub.2 OEt    Ga                                                    CH.sub.2 CH.sub.2 OPr-n  Gb                                                    CH.sub.2 CHMeOMe         Gb                                                    CH.sub.2 CH.sub.2 CH.sub.2 OMe                                                                          Ga                                                    CH.sub.2 CH.sub.2 CH.sub.2 OEt                                                                          Ga                                                    CH.sub.2 OCH.sub.2 CHCH.sub.2                                                                           Ga                                                    CH.sub.2 OCH.sub.2 CHCHMe                                                                               Ga                                                    CH.sub.2 CH.sub.2 OCH.sub.2 CHCH.sub.2                                                                  Ga                                                    CH.sub.2 CH.sub.2 OCH.sub.2 CHCHMe                                                                      Ga                                                    CH.sub.2 OCH.sub.2 CCH   Ga                                                    CH.sub.2 OCH.sub.2 CCMe  Ga                                                    CH.sub.2 CH.sub.2 OCH.sub.2 CCH                                                                         Ga                                                    CH.sub.2 CH.sub.2 OCH.sub.2 CCMe                                                                        Ga                                                    CH.sub.2 OCHF.sub.2      Ga                                                    CH.sub.2 OCF.sub.3       Ga                                                    CH.sub.2 CH.sub.2 OCHF.sub.2                                                                            Ga                                                    CH.sub.2 CH.sub.2 OCF.sub.3                                                                             Ga                                                    CH.sub.2 OCH.sub.2 CF.sub.3                                                                             Ga                                                    CH.sub.2 CH.sub.2 OCH.sub.2 CF.sub.3                                                                    Ga                                                    CH.sub.2 OCH.sub.2 CH.sub.2 F                                                                           Ga                                                    CH.sub.2 OCH.sub.2 CH.sub.2 Cl                                                                          Ga                                                    CH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 F                                                                  Ga                                                    CH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 Cl                                                                 Ga                                                    CH.sub.2 OCH.sub.2 CHCHCl                                                                               Gb                                                    CH.sub.2 CH.sub.2 OCH.sub.2 CHCHCl                                                                      Gb                                                    CH.sub.2 OCH.sub.2 CHCHBr                                                                               Gb                                                    CH.sub.2 CH.sub.2 OCH.sub.2 CHCHBr                                                                      Gb                                                    CH.sub.2 OCH.sub.2 CHCF.sub.2                                                                           Gb                                                    CH.sub.2 CH.sub.2 OCH.sub.2 CHCF.sub.2                                                                  Gb                                                    CH.sub.2 OCH.sub.2 CHCHCF.sub.3                                                                         Gb                                                    CH.sub.2 CH.sub.2 OCH.sub.2 CHCHCF.sub.3                                                                Gb                                                    CH.sub.2 OCH.sub.2 CCI   Gb                                                    CH.sub.2 CH.sub.2 OCH.sub.2 CCI                                                                         Gb                                                    CH.sub.2 OCH.sub.2 CCCF.sub.3                                                                           Gb                                                    CH.sub.2 CH.sub.2 OCH.sub.2 CCCF.sub.3                                                                  Gb                                                    CH.sub.2 SMe             Ga                                                    CH.sub.2 SEt             Ga                                                    CH.sub.2 SPr-n           Gb                                                    CH.sub.2 CH.sub.2 SMe    Ga                                                    CH.sub.2 CH.sub.2 SEt    Ga                                                    CH.sub.2 CH.sub.2 SPr-n  Gb                                                    CH.sub.2 SOMe            Gb                                                    CH.sub.2 SOEt            Gb                                                    CH.sub.2 CH.sub.2 SOMe   Gb                                                    CH.sub.2 CH.sub.2 SOEt   Gb                                                    CH.sub.2 SO.sub.2 Me     Ga                                                    CH.sub.2 SO.sub.2 Et     Ga                                                    CH.sub.2 SO.sub.2 Pr-n   Gb                                                    CH.sub.2 CH.sub.2 SO.sub.2 Me                                                                           Ga                                                    CH.sub.2 CH.sub.2 SO.sub.2 Et                                                                           Ga                                                    CH.sub.2 CH.sub.2 SO.sub.2 Pr-n                                                                         Gb                                                    CH.sub.2 CH.sub.2 F      Ga                                                    CH.sub.2 CHF.sub.2       Ga                                                    CH.sub.2 CF.sub.3        Ga                                                    CH.sub.2 CH.sub.2 Cl     Ga                                                    CH.sub.2 CH.sub.2 Br     Ga                                                    CH.sub.2 CH.sub.2 CF.sub.3                                                                              Ga                                                    CH.sub.2 CF.sub.2 CF.sub.3                                                                              Ga                                                    CH.sub.2 CHCHCl          Ga                                                    CH.sub.2 CHCHBr          Ga                                                    CH.sub.2 CHCF.sub.2      Ga                                                    CH.sub.2 CHCHCF.sub.3    Ga                                                    CH.sub.2 CCI             Gb                                                    CH.sub.2 CCCF.sub.3      Gb                                                    CH.sub.2 CN              Ga                                                    CH.sub.2 CH.sub.2 CN     Ga                                                    CHMeCN                   Ga                                                    CH.sub.2 CHCHCN          Ga                                                    CH(CN)CCH                Gb                                                    CH.sub.2 NO.sub.2        Ga                                                    CH.sub.2 CH.sub.2 NO.sub.2                                                                              Ga                                                    CH.sub.2 CHCHNO.sub.2    Gb                                                    CH.sub.2 CH(NO.sub.2)CHCH.sub.2                                                                         Gc                                                    CH.sub.2 CH(NO.sub.2)CCH Gc                                                    CH.sub.2 CO.sub.2 Me     Gb                                                    CH.sub.2 CO.sub.2 Et     Gb                                                    CH.sub.2 CO.sub.2 Pr-n   Gb                                                    CHMeCO.sub.2 Me          Gb                                                    CHMeCO.sub.2 Et          Gb                                                    CH.sub.2 CH.sub.2 CO.sub.2 Me                                                                           Ga                                                    CH.sub.2 CH.sub.2 CO.sub.2 Et                                                                           Ga                                                    CH.sub.2 CH.sub.2 CH.sub.2 CO.sub.2 Me                                                                  Gb                                                    CH.sub.2 CHCHCO.sub.2 Me Ga                                                    CH.sub.2 CHCHCO.sub.2 Et Ga                                                    CHMeCHCHCO.sub.2 Me      Ga                                                    CHMeCHCHCO.sub.2 Et      Ga                                                    CH.sub.2 CCCO.sub.2 Me   Ga                                                    CH.sub.2 CCCO.sub.2 Et   Ga                                                    CH.sub.2 COMe            Ga                                                    CH.sub.2 COEt            Ga                                                    CH.sub.2 COPr-n          Gb                                                    CH.sub.2 CH.sub.2 COMe   Ga                                                    CH.sub.2 CH.sub.2 COEt   Ga                                                    CH.sub.2 COCF.sub.3      Ga                                                    CH.sub.2 CH.sub.2 COCF.sub.3                                                                            Ga                                                    CH.sub.2 COCH.sub.2 CF.sub.3                                                                            Gb                                                    CH.sub.2 COCH.sub.2 F    Gb                                                    CH.sub.2 COCHCH.sub.2    Ga                                                    CH.sub.2 COCHCHMe        Ga                                                    CH.sub.2 COCH.sub.2 CHCH.sub.2                                                                          Gb                                                    CH.sub.2 CH.sub.2 COCHCH.sub.2                                                                          Gb                                                    CH.sub.2 CH.sub.2 COCHCHMe                                                                              Gb                                                    CH.sub.2 COCCH           Ga                                                    CH.sub.2 COCCMe          Ga                                                    CH.sub.2 COCH.sub.2 OMe  Ga                                                    CH.sub.2 COCH.sub.2 OEt  Ga                                                    CH.sub.2 COCH.sub.2 CH.sub.2 OMe                                                                        Ga                                                    CH.sub.2 COCH.sub.2 CH.sub.2 OEt                                                                        Ga                                                    CH.sub.2 COCH.sub.2 SMe  Ga                                                    CH.sub.2 COCH.sub.2 SEt  Ga                                                    CH.sub.2 COCH.sub.2 CH.sub.2 SMe                                                                        Ga                                                    CH.sub.2 COCH.sub.2 CH.sub.2 SEt                                                                        Ga                                                    CH.sub.2 COCH.sub.2 SOMe Gb                                                    CH.sub.2 COCH.sub.2 CH.sub.2 SOMe                                                                       Gb                                                    CH.sub.2 COCH.sub.2 SO.sub.2 Me                                                                         Ga                                                    CH.sub.2 COCH.sub.2 SO.sub.2 Et                                                                         Ga                                                    CH.sub.2 COCH.sub.2 CH.sub.2 SO.sub.2 Me                                                                Ga                                                    CH.sub.2 COCH.sub.2 CH.sub.2 SO.sub.2 Et                                                                Ga                                                    CH.sub.2 CHCHCOMe        Ga                                                    CH.sub.2 CHCHCOEt        Ga                                                    CHMeCHCHCOMe             Ga                                                    CHMeCHCHCOEt             Ga                                                    CH.sub.2 CCCOMe          Ga                                                    CH.sub.2 CCCOEt          Ga                                                    CH.sub.2 SO.sub.2 NHMe   Ga                                                    CH.sub.2 SO.sub.2 NHEt   Ga                                                    CH.sub.2 CH.sub.2 SO.sub.2 NHMe                                                                         Ga                                                    CH.sub.2 CH.sub.2 SO.sub.2 NHEt                                                                         Ga                                                    CH.sub.2 SO.sub.2 NHOMe  Ga                                                    CH.sub.2 SO.sub.2 NHOEt  Ga                                                    CH.sub.2 CH.sub.2 SO.sub.2 NHOMe                                                                        Ga                                                    CH.sub.2 CH.sub.2 SO.sub.2 NHOEt                                                                        Ga                                                    CH.sub.2 SO.sub.2 NMe.sub.2                                                                             Ga                                                    CH.sub.2 SO.sub.2 NMeEt  Ga                                                    CH.sub.2 SO.sub.2 NEt    Ga                                                    CH.sub.2 CH.sub.2 SO.sub.2 NMe.sub.2                                                                    Ga                                                    CH.sub.2 CH.sub.2 SO.sub.2 NMeEt                                                                        Ga                                                    CH.sub.2 CH.sub.2 SO.sub.2 NEt.sub.2                                                                    Ga                                                    CH.sub.2 SO.sub.2 N(OMe)Me                                                                              Ga                                                    CH.sub.2 SO.sub.2 N(OMe)Et                                                                              Ga                                                    CH.sub.2 SO.sub.2 N(OEt)Me                                                                              Ga                                                    CH.sub.2 CH.sub.2 SO.sub.2 N(OMe)Me                                                                     Ga                                                    CH.sub.2 CH.sub.2 SO.sub.2 N(OMe)Et                                                                     Ga                                                    CH.sub.2 CH.sub.2 SO.sub.2 N(OEt)Me                                                                     Ga                                                    CH.sub.2 CONHMe          Ga                                                    CH.sub.2 CONHEt          Ga                                                    CH.sub.2 CONHPr-n        Gb                                                    CH.sub.2 CH.sub.2 CONHMe Ga                                                    CH.sub.2 CH.sub.2 CONHEt Ga                                                    CH.sub.2 CH.sub.2 CONHPr-n                                                                              Gb                                                    CH.sub.2 CONMe.sub.2     Ga                                                    CH.sub.2 CONMeEt         Ga                                                    CH.sub.2 CONEt.sub.2     Ga                                                    CH.sub.2 CONHOMe         Ga                                                    CH.sub.2 CONHOEt         Ga                                                    CH.sub.2 CONHOPr-n       Gb                                                    CH.sub.2 CON(OMe)Me      Ga                                                    CH.sub.2 CON(OMe)Et      Ga                                                    CH.sub.2 CON(OEt)Me      Ga                                                    CH.sub.2 CON(OEt)Et      Ga                                                    CH.sub.2 NHMe            Ga                                                    CH.sub.2 NHEt            Ga                                                    CH.sub.2 NHPr-n          Gb                                                    CH.sub.2 CH.sub.2 NHMe   Ga                                                    CH.sub.2 CH.sub.2 NHEt   Ga                                                    CH.sub.2 CH.sub.2 NHPr-n Gb                                                    CH.sub.2 NHOMe           Ga                                                    CH.sub.2 NHOEt           Ga                                                    CH.sub.2 CH.sub.2 NHOMe  Ga                                                    CH.sub.2 CH.sub.2 NHOEt  Ga                                                    CH.sub.2 NMe.sub.2       Ga                                                    CH.sub.2 NMeEt           Ga                                                    CH.sub.2 CH.sub.2 NMe.sub.2                                                                             Ga                                                    CH.sub.2 CH.sub.2 NMeEt  Ga                                                    CH.sub.2 N(OMe)Me        Ga                                                    CH.sub.2 N(OMe)Et        Ga                                                    CH.sub.2 N(OEt)Me        Ga                                                    CH.sub.2 CH.sub.2 N(OMe)Me                                                                              Ga                                                    CH.sub.2 CH.sub.2 N(OMe)Et                                                                              Ga                                                    CH.sub.2 CH.sub.2 N(OEt)Me                                                                              Ga                                                    CH.sub.2 NMeCOMe         Ga                                                    CH.sub.2 NEtCOMe         Ga                                                    CH.sub.2 NMeCOEt         Ga                                                    CH.sub.2 CH.sub.2 NMeCOMe                                                                               Ga                                                    CH.sub.2 CH.sub.2 NEtCOMe                                                                               Ga                                                    CH.sub.2 CH.sub.2 NMeCOEt                                                                               Ga                                                    CH.sub.2 N(OMe)COMe      Ga                                                    CH.sub.2 N(OEt)COMe      Ga                                                    CH.sub.2 N(OMe)COEt      Ga                                                    CH.sub.2 CH.sub.2 N(OMe)COMe                                                                            Ga                                                    CH.sub.2 CH.sub.2 N(OEt)COMe                                                                            Ga                                                    CH.sub.2 CH.sub.2 N(OMe)COEt                                                                            Ga                                                    CH.sub.2 NMeSO.sub.2 Me  Ga                                                    CH.sub.2 NEtSO.sub.2 Me  Ga                                                    CH.sub.2 NMeSO.sub.2 Et  Ga                                                    CH.sub.2 CH.sub.2 NMeSO.sub.2 Me                                                                        Ga                                                    CH.sub.2 CH.sub.2 NEtSO.sub.2 Me                                                                        Ga                                                    CH.sub.2 CH.sub.2 NMeSO.sub.2 Et                                                                        Ga                                                    CH.sub.2 N(OMe)SO.sub.2 Me                                                                              Ga                                                    CH.sub.2 N(OEt)SO.sub.2 Me                                                                              Ga                                                    CH.sub.2 N(OMe)SO.sub.2 Et                                                                              Ga                                                    CH.sub.2 CH.sub.2 N(OMe)SO.sub.2 Me                                                                     Ga                                                    CH.sub.2 CH.sub.2 N(OEt)SO.sub.2 Me                                                                     Ga                                                    CH.sub.2 CH.sub.2 N(OMe)SO.sub.2 Et                                                                     Ga                                                    CH.sub.2 Ph              Gb                                                    CH.sub.2 CH.sub.2 Ph     Gb                                                    CH.sub.2 CH.sub.2 CH.sub.2 Ph                                                                           Gb                                                    CHMePh                   Gb                                                    CH.sub.2 CHCHPh          Ga                                                    CHMeCHCHPh               Ga                                                    CH.sub.2 CCPh            Ga                                                    CHMeCCPh                 Ga                                                    CH.sub.2 CH.sub.2 OPh    Ga                                                    CH.sub.2 OPh             Ga                                                    CH.sub.2 CH.sub.2 SPh    Ga                                                    CH.sub.2 SPh             Ga                                                    CH.sub.2 CH.sub.2 SOPh   Gb                                                    CH.sub.2 CH.sub.2 SO.sub.2 Ph                                                                           Ga                                                    CH.sub.2 OCH.sub.2 Ph    Ga                                                    CH.sub.2 CH.sub.2 OCH.sub.2 Ph                                                                          Ga                                                    CH.sub.2 SCH.sub.2 Ph    Ga                                                    CH.sub.2 CH.sub.2 SCH.sub.2 Ph                                                                          Ga                                                    CH.sub.2 SOCH.sub.2 Ph   Gb                                                    CH.sub.2 CH.sub.2 SOCH.sub.2 Ph                                                                         Gb                                                    CH.sub.2 SO.sub.2 CH.sub.2 Ph                                                                           Ga                                                    CH.sub.2 CH.sub.2 SO.sub.2 CH.sub.2 Ph                                                                  Ga                                                    CH.sub.2 COPh            Ga                                                    CH.sub.2 CH.sub.2 COPh   Ga                                                    CHMeCOPh                 Ga                                                    CH.sub.2 COCH.sub.2 Ph   Gb                                                    CHMeCOCH.sub.2 Ph        Gb                                                    CH.sub.2 CH.sub.2 CH.sub.2 F                                                                            Ga                                                    CH.sub.2 CH.sub.2 CH.sub.2 Cl                                                                           Ga                                                    CH.sub.2 C(Cl)CH.sub.2   Ga                                                    CH.sub.2 C(Br)CH.sub.2   Ga                                                    Ph                       Ga                                                    CH.sub.2 SOPh            Ga                                                    CH.sub.2 SO.sub.2 Ph     Ga                                                    CH.sub.2 Ph-4-OMe        Gb                                                    CH.sub.2 Ph-4-Cl         Gb                                                    CH.sub.2 C(Cl)CHCl       Ga                                                    CH.sub.2 C(F)CHCl        Ga                                                    CH.sub.2 CHCHF           Ga                                                    CH.sub.2 C(Cl)CHMe       Ga                                                    CH.sub.2 CHC(Cl)Me       Ga                                                    CH.sub.2 CFCF.sub.2      Ga                                                    CH.sub.2 CHCHCH.sub.2 F  Ga                                                    CH.sub.2 C(Br)CHMe       Ga                                                    CH.sub.2 C(Cl)CHF        Ga                                                    CH.sub.2 C(Br)CHF        Ga                                                    CH.sub.2 C(Cl)C(Cl)Me    Ga                                                    CH.sub.2 C(Br)CHBr       Ga                                                    CH.sub.2 C(Br)C(Br)Me    Ga                                                    CH.sub.2 CHC(F)CF.sub.3  Ga                                                    CH.sub.2 CHCCl.sub.2     Ga                                                    CH.sub.2 C(F)CH.sub.2    Ga                                                    CH.sub.2 CHC(F)Cl        Ga                                                    CH.sub.2 C(Cl)C(F)Cl     Ga                                                    CH.sub.2 C(F)CCl.sub.2   Ga                                                    CH.sub.2 CClCF.sub.2     Ga                                                    CH.sub.2 C(CF.sub.3)CH.sub.2                                                                            Ga                                                    CH.sub.2 NHSO.sub.2 Me   Gb                                                    CH.sub.2 CH.sub.2 NHSO.sub.2 Me                                                                         Gb                                                    CH.sub.2 NHCOMe          Gb                                                    CH.sub.2 CH.sub.2 NHCOMe Gb                                                    ______________________________________                                    

                  TABLE 1B                                                         ______________________________________                                          ##STR115##                                                                    Q:                                                                              ##STR116##                                                                     ##STR117##                                                                     ##STR118##                                                                     ##STR119##                                                                     ##STR120##                                                                     ##STR121##                                                                     ##STR122##                                                                     ##STR123##                                                                     ##STR124##                                                                     ##STR125##                                                                     ##STR126##                                                                     ##STR127##                                                                     ##STR128##                                                                     ##STR129##                                                                     ##STR130##                                                                     ##STR131##                                                                     ##STR132##                                                                     ##STR133##                                                                     ##STR134##                                                                     ##STR135##                                                                     ##STR136##                                                                     ##STR137##                                                                     ##STR138##                                                                     ##STR139##                                                                     ##STR140##                                                                     ##STR141##                                                                     ##STR142##                                                                     ##STR143##                                                                     ##STR144##                                                                     ##STR145##                                                                     ##STR146##                                                                     ##STR147##                                                                     ##STR148##                                                                     ##STR149##                                                                     ##STR150##                                                                     ##STR151##                                                                     ##STR152##                                                                     ##STR153##                                                                     ##STR154##                                                                     ##STR155##                                                                     ##STR156##                                                                     ##STR157##                                                                     ##STR158##                                                                     ##STR159##                                                                     ##STR160##                                                                     ##STR161##                                                                     ##STR162##                                                                     ##STR163##                                                                     ##STR164##                                                                     ##STR165##                                                                     ##STR166##                                                                     ##STR167##                                                                     ##STR168##                                                                     ##STR169##                                                                     ##STR170##                                                                     ##STR171##                                                                     ##STR172##                                                                     ##STR173##                                                                     ##STR174##                                                                     ##STR175##                                                                     ##STR176##                                                                     ##STR177##                                                                     ##STR178##                                                                     ##STR179##                                                                     ##STR180##                                                                     ##STR181##                                                                     ##STR182##                                                                     ##STR183##                                                                     ##STR184##                                                                     ##STR185##                                                                     ##STR186##                                                                     ##STR187##                                                                     ##STR188##                                                                     ##STR189##                                                                     ##STR190##                                                                     ##STR191##                                                                     ##STR192##                                                                     ##STR193##                                                                     ##STR194##                                                                     ##STR195##                                                                     ##STR196##                                                                     ##STR197##                                                                     ##STR198##                                                                     ##STR199##                                                                     ##STR200##                                                                     ##STR201##                                                                     ##STR202##                                                                     ##STR203##                                                                     ##STR204##                                                                     ##STR205##                                                                     ##STR206##                                                                     ##STR207##                                                                     ##STR208##                                                                     ##STR209##                                                                     ##STR210##                                                                     ##STR211##                                                                     ##STR212##                                                                     ##STR213##                                                                     ##STR214##                                                                     ##STR215##                                                                     ##STR216##                                                                     ##STR217##                                                                     ##STR218##                                                                     ##STR219##                                                                     ##STR220##                                                                     ##STR221##                                                                     ##STR222##                                                                     ##STR223##                                                                     ##STR224##                                                                     ##STR225##                                                                     ##STR226##                                                                     ##STR227##                                                                     ##STR228##                                                                     ##STR229##                                                                     ##STR230##                                                                     ##STR231##                                                                     ##STR232##                                                                     ##STR233##                                                                     ##STR234##                                                                     ##STR235##                                                                     ##STR236##                                                                     ##STR237##                                                                     ##STR238##                                                                     ##STR239##                                                                     ##STR240##                                                                     ##STR241##                                                                     ##STR242##                                                                     ##STR243##                                                                     ##STR244##                                                                     ##STR245##                                                                     ##STR246##                                                                     ##STR247##                                                                     ##STR248##                                                                     ##STR249##                                                                     ##STR250##                                                                     ##STR251##                                                                     ##STR252##                                                                     ##STR253##                                                                     ##STR254##                                                                     ##STR255##                                                                     ##STR256##                                                                     ##STR257##                                                                     ##STR258##                                                                     ##STR259##                                                                     ##STR260##                                                                     ##STR261##                                                                     ##STR262##                                                                     ##STR263##                                                                     ##STR264##                                                                     ##STR265##                                                                     ##STR266##                                                                     ##STR267##                                                                     ##STR268##                                                                     ##STR269##                                                                     ##STR270##                                                                     ##STR271##                                                                     ##STR272##                                                                     ##STR273##                                                                     ##STR274##                                                                     ##STR275##                                                                     ##STR276##                                                                     ##STR277##                                                                     ##STR278##                                                                     ##STR279##                                                                     ##STR280##                                                                     ##STR281##                                                                     ##STR282##                                                                     ##STR283##                                                                     ##STR284##                                                                     ##STR285##                                                                     ##STR286##                                                                     ##STR287##                                                                     ##STR288##                                                                     ##STR289##                                                                     ##STR290##                                                                     ##STR291##                                                                     ##STR292##                                                                     ##STR293##                                                                     ##STR294##                                                                     ##STR295##                                                                     ##STR296##                                                                     ##STR297##                                                                     ##STR298##                                                                     ##STR299##                                                                     ##STR300##                                                                     ##STR301##                                                                     ##STR302##                                                                     ##STR303##                                                                     ##STR304##                                                                     ##STR305##                                                                     ##STR306##                                                                     ##STR307##                                                                     ##STR308##                                                                     ##STR309##                                                                     ##STR310##                                                                     ##STR311##                                                                     ##STR312##                                                                     ##STR313##                                                                     ##STR314##                                                                     ##STR315##                                                                     ##STR316##                                                                     ##STR317##                                                                     ##STR318##                                                                     ##STR319##                                                                     ##STR320##                                                                     ##STR321##                                                                     ##STR322##                                                                     ##STR323##                                                                     ##STR324##                                                                     ##STR325##                                                                     ##STR326##                                                                     ##STR327##                                                                     ##STR328##                                                                     ##STR329##                                                                     ##STR330##                                                                     ##STR331##                                                                     ##STR332##                                                                     ##STR333##                                                                     ##STR334##                                                                     ##STR335##                                                                     ##STR336##                                                                     ##STR337##                                                                     ##STR338##                                                                     ##STR339##                                                                     ##STR340##                                                                     ##STR341##                                                                     ##STR342##                                                                     ##STR343##                                                                     ##STR344##                                                                     ##STR345##                                                                     ##STR346##                                                                     ##STR347##                                                                     ##STR348##                                                                     ##STR349##                                                                     ##STR350##                                                                     ##STR351##                                                                     ##STR352##                                                                     ##STR353##                                                                     ##STR354##                                                                     ##STR355##                                                                     ##STR356##                                                                     ##STR357##                                                                     ##STR358##                                                                     ##STR359##                                                                     ##STR360##                                                                     ##STR361##                                                                     ##STR362##                                                                     ##STR363##                                                                     ##STR364##                                                                     ##STR365##                                                                     ##STR366##                                                                     ##STR367##                                                                     ##STR368##                                                                     ##STR369##                                                                     ##STR370##                                                                     ##STR371##                                                                     ##STR372##                                                                     ##STR373##                                                                     ##STR374##                                                                     ##STR375##                                                                     ##STR376##                                                                     ##STR377##                                                                     ##STR378##                                                                     ##STR379##                                                                     ##STR380##                                                                     ##STR381##                                                                     ##STR382##                                                                     ##STR383##                                                                     ##STR384##                                                                     ##STR385##                                                                     ##STR386##                                                                     ##STR387##                                                                     ##STR388##                                                                     ##STR389##                                                                     ##STR390##                                                                     ##STR391##                                                                     ##STR392##                                                                     ##STR393##                                                                     ##STR394##                                                                     ##STR395##                                                                     ##STR396##                                                                     ##STR397##                                                                     ##STR398##                                                                     ##STR399##                                                                     ##STR400##                                                                     ##STR401##                                                                     ##STR402##                                                                     ##STR403##                                                                     ##STR404##                                                                     ##STR405##                                                                     ##STR406##                                                                    R.sup.m represents R.sup.a1, R.sup.b1, R.sup.d1, R.sup.e1 or                   ______________________________________                                         R.sup.f1.                                                                      R.sup.m                       Gn                                               ______________________________________                                         Me                            Ga                                               Et                            Ga                                               Pr-n                          Ga                                               Pr-iso                        Ga                                               Bu-n                          Ga                                               Bu-iso                        Gb                                               Pen-n                         Gb                                               Hex-n                         Gb                                               CH.sub.2 Pr-cyc               Ga                                               CH.sub.2 CH.sub.2 Pr-cyc      Ga                                               CH.sub.2 CHCH.sub.2           Ga                                               CH.sub.2 CHCHMe               Ga                                               CH.sub.2 CCH                  Ga                                               CH.sub.2 CCMe                 Ga                                               CH.sub.2 OMe                  Ga                                               CH.sub.2 OEt                  Ga                                               CH.sub.2 CH.sub.2 OMe         Ga                                               CH.sub.2 CH.sub.2 OEt         Ga                                               CH.sub.2 OCH.sub.2 CHCH.sub.2 Ga                                               CH.sub.2 CH.sub.2 OCH.sub.2 CHCH.sub.2                                                                       Ga                                               CH.sub.2 OCH.sub.2 CCH        Ga                                               CH.sub.2 CH.sub.2 OCH.sub.2 CCH                                                                              Ga                                               CH.sub.2 OCH.sub.2 CF.sub.3   Ga                                               CH.sub.2 CH.sub.2 OCH.sub.2 CF.sub.3                                                                         Ga                                               CH.sub.2 SMe                  Ga                                               CH.sub.2 SEt                  Ga                                               CH.sub.2 CH.sub.2 SMe         Ga                                               CH.sub.2 CH.sub.2 SEt         Ga                                               CH.sub.2 SO.sub.2 Me          Ga                                               CH.sub.2 SO.sub.2 Et          Ga                                               CH.sub.2 CH.sub.2 SO.sub.2 Me Ga                                               CH.sub.2 CH.sub.2 SO.sub.2 Et Ga                                               CH.sub.2 CH.sub.2 F           Ga                                               CH.sub.2 CF.sub.3             Ga                                               CH.sub.2 CN                   Ga                                               CH.sub.2 CH.sub.2 CN          Ga                                               CHMeCN                        Ga                                               CH.sub.2 CHCHCN               Ga                                               CH.sub.2 NO.sub.2             Ga                                               CH.sub.2 CH.sub.2 NO.sub.2    Ga                                               CH.sub.2 CO.sub.2 Me          Gb                                               CH.sub.2 CO.sub.2 Et          Gb                                               CHMeCO.sub.2 Me               Gb                                               CHMeCO.sub.2 Et               Gb                                               CH.sub.2 CH.sub.2 CO.sub.2 Me Ga                                               CH.sub.2 CH.sub.2 CO.sub.2 Et Ga                                               CH.sub.2 CHCHCO.sub.2 Me      Ga                                               CH.sub.2 CHCHCO.sub.2 Et      Ga                                               CHMeCHCHCO.sub.2 Me           Ga                                               CH.sub.2 COMe                 Ga                                               CH.sub.2 COEt                 Ga                                               CH.sub.2 COPr-n               Gb                                               CH.sub.2 COCF.sub.3           Ga                                               CH.sub.2 COCHCH.sub.2         Ga                                               CH.sub.2 COCHCHMe             Ga                                               CH.sub.2 COCH.sub.2 OMe       Ga                                               CH.sub.2 COCH.sub.2 OEt       Ga                                               CH.sub.2 COCH.sub.2 CH.sub.2 OMe                                                                             Ga                                               CH.sub.2 COCH.sub.2 CH.sub.2 OEt                                                                             Ga                                               CH.sub.2 COCH.sub.2 SMe       Ga                                               CH.sub.2 COCH.sub.2 CH.sub.2 SMe                                                                             Ga                                               CH.sub.2 COCH.sub.2 SO.sub.2 Me                                                                              Ga                                               CH.sub.2 COCH.sub.2 CH.sub.2 SO.sub.2 Me                                                                     Ga                                               CH.sub.2 CHCHCOMe             Ga                                               CHMeCHCHCOMe                  Ga                                               CH.sub.2 SO.sub.2 NHMe        Gb                                               CH.sub.2 CH.sub.2 SO.sub.2 NHMe                                                                              Gb                                               CH.sub.2 SO.sub.2 NHOMe       Gb                                               CH.sub.2 CH.sub.2 SO.sub.2 NHOMe                                                                             Gb                                               CH.sub.2 SO.sub.2 NMe.sub.2   Ga                                               CH.sub.2 CH.sub.2 SO.sub.2 NMe.sub.2                                                                         Ga                                               CH.sub.2 SO.sub.2 N(OMe)Me    Ga                                               CH.sub.2 CH.sub.2 SO.sub.2 N(OMe)Me                                                                          Ga                                               CH.sub.2 CONHMe               Gb                                               CH.sub.2 CH.sub.2 CONHMe      Gb                                               CH.sub.2 CONMe.sub.2          Ga                                               CH.sub.2 CH.sub.2 CONMe.sub.2 Ga                                               CH.sub.2 CONHOMe              Gb                                               CH.sub.2 CH.sub.2 CONHOMe     Gb                                               CH.sub.2 CON(OMe)Me           Ga                                               CH.sub.2 CH.sub.2 CON(OMe)Me  Ga                                               CH.sub.2 NHMe                 Gb                                               CH.sub.2 CH.sub.2 NHMe        Gb                                               CH.sub.2 NHOMe                Gb                                               CH.sub.2 CH.sub.2 NHOMe       Gb                                               CH.sub.2 NMe.sub.2            Ga                                               CH.sub.2 CH.sub.2 NMe.sub.2   Ga                                               CH.sub.2 N(OMe)Me             Ga                                               CH.sub.2 CH.sub.2 N(OMe)Me    Ga                                               CH.sub.2 NMeCOMe              Ga                                               CH.sub.2 CH.sub.2 NMeCOMe     Ga                                               CH.sub.2 N(OMe)COMe           Ga                                               CH.sub.2 CH.sub.2 N(OMe)COMe  Ga                                               CH.sub.2 NMeSO.sub.2 Me       Ga                                               CH.sub.2 CH.sub.2 NMeSO.sub.2 Me                                                                             Ga                                               CH.sub.2 N(OMe)SO.sub.2 Me    Ga                                               CH.sub.2 CH.sub.2 N(OMe)SO.sub.2 Me                                                                          Ga                                               CH.sub.2 Ph                   Gb                                               CH.sub.2 CH.sub.2 Ph          Gb                                               CH.sub.2 CH.sub.2 CH.sub.2 Ph Gb                                               CHMePh                        Gb                                               CH.sub.2 CHCHPh               Gb                                               CHMeCHCHPh                    Gb                                               CH.sub.2 CH.sub.2 OPh         Gb                                               CH.sub.2 OPh                  Gb                                               CH.sub.2 CH.sub.2 SPh         Gb                                               CH.sub.2 SPh                  Gb                                               CH.sub.2 CH.sub.2 SO.sub.2 Ph Gb                                               CH.sub.2 COPh                 Gb                                               CH.sub.2 CH.sub.2 COPh        Gb                                               CH.sub.2 COCH.sub.2 Ph        Gb                                               CH.sub.2 CH.sub.2 COCH.sub.2 Ph                                                                              Gb                                               Ph                            Gb                                               ______________________________________                                    

                  TABLE 1C                                                         ______________________________________                                          ##STR407##                                                                    Q:                                                                              ##STR408##                                                                     ##STR409##                                                                     ##STR410##                                                                     ##STR411##                                                                     ##STR412##                                                                     ##STR413##                                                                     ##STR414##                                                                     ##STR415##                                                                     ##STR416##                                                                     ##STR417##                                                                     ##STR418##                                                                     ##STR419##                                                                     ##STR420##                                                                     ##STR421##                                                                     ##STR422##                                                                     ##STR423##                                                                     ##STR424##                                                                     ##STR425##                                                                     ##STR426##                                                                     ##STR427##                                                                     ##STR428##                                                                     ##STR429##                                                                     ##STR430##                                                                     ##STR431##                                                                     ##STR432##                                                                     ##STR433##                                                                     ##STR434##                                                                     ##STR435##                                                                     ##STR436##                                                                     ##STR437##                                                                     ##STR438##                                                                     ##STR439##                                                                     ##STR440##                                                                     ##STR441##                                                                     ##STR442##                                                                     ##STR443##                                                                     ##STR444##                                                                     ##STR445##                                                                     ##STR446##                                                                     ##STR447##                                                                     ##STR448##                                                                     ##STR449##                                                                     ##STR450##                                                                     ##STR451##                                                                     ##STR452##                                                                     ##STR453##                                                                     ##STR454##                                                                     ##STR455##                                                                     ##STR456##                                                                     ##STR457##                                                                     ##STR458##                                                                     ##STR459##                                                                     ##STR460##                                                                     ##STR461##                                                                     ##STR462##                                                                     ##STR463##                                                                     ##STR464##                                                                     ##STR465##                                                                     ##STR466##                                                                     ##STR467##                                                                     ##STR468##                                                                     ##STR469##                                                                     ##STR470##                                                                     ##STR471##                                                                     ##STR472##                                                                     ##STR473##                                                                     ##STR474##                                                                     ##STR475##                                                                     ##STR476##                                                                     ##STR477##                                                                     ##STR478##                                                                     ##STR479##                                                                     ##STR480##                                                                     ##STR481##                                                                     ##STR482##                                                                     ##STR483##                                                                     ##STR484##                                                                     ##STR485##                                                                     ##STR486##                                                                     ##STR487##                                                                     ##STR488##                                                                     ##STR489##                                                                     ##STR490##                                                                     ##STR491##                                                                     ##STR492##                                                                     ##STR493##                                                                     ##STR494##                                                                     ##STR495##                                                                     ##STR496##                                                                     ##STR497##                                                                     ##STR498##                                                                     ##STR499##                                                                     ##STR500##                                                                     ##STR501##                                                                     ##STR502##                                                                     ##STR503##                                                                     ##STR504##                                                                     ##STR505##                                                                     ##STR506##                                                                     ##STR507##                                                                     ##STR508##                                                                     ##STR509##                                                                     ##STR510##                                                                     ##STR511##                                                                     ##STR512##                                                                     ##STR513##                                                                     ##STR514##                                                                     ##STR515##                                                                     ##STR516##                                                                     ##STR517##                                                                     ##STR518##                                                                     ##STR519##                                                                     ##STR520##                                                                     ##STR521##                                                                     ##STR522##                                                                     ##STR523##                                                                     ##STR524##                                                                     ##STR525##                                                                     ##STR526##                                                                     ##STR527##                                                                     ##STR528##                                                                     ##STR529##                                                                     ##STR530##                                                                     ##STR531##                                                                     ##STR532##                                                                     ##STR533##                                                                     ##STR534##                                                                     ##STR535##                                                                     ##STR536##                                                                     ##STR537##                                                                     ##STR538##                                                                     ##STR539##                                                                     ##STR540##                                                                     ##STR541##                                                                     ##STR542##                                                                     ##STR543##                                                                     ##STR544##                                                                     ##STR545##                                                                     ##STR546##                                                                     ##STR547##                                                                     ##STR548##                                                                     ##STR549##                                                                     ##STR550##                                                                     ##STR551##                                                                     ##STR552##                                                                     ##STR553##                                                                     ##STR554##                                                                     ##STR555##                                                                     ##STR556##                                                                     ##STR557##                                                                     ##STR558##                                                                     ##STR559##                                                                     ##STR560##                                                                     ##STR561##                                                                     ##STR562##                                                                     ##STR563##                                                                     ##STR564##                                                                     ##STR565##                                                                     ##STR566##                                                                     ##STR567##                                                                     ##STR568##                                                                     ##STR569##                                                                     ##STR570##                                                                     ##STR571##                                                                     ##STR572##                                                                     ##STR573##                                                                     ##STR574##                                                                     ##STR575##                                                                     ##STR576##                                                                     ##STR577##                                                                     ##STR578##                                                                     ##STR579##                                                                     ##STR580##                                                                     ##STR581##                                                                     ##STR582##                                                                     ##STR583##                                                                     ##STR584##                                                                     ##STR585##                                                                     ##STR586##                                                                     ##STR587##                                                                     ##STR588##                                                                     ##STR589##                                                                     ##STR590##                                                                     ##STR591##                                                                     ##STR592##                                                                     ##STR593##                                                                     ##STR594##                                                                     ##STR595##                                                                     ##STR596##                                                                     ##STR597##                                                                     ##STR598##                                                                     ##STR599##                                                                     ##STR600##                                                                     ##STR601##                                                                     ##STR602##                                                                     ##STR603##                                                                     ##STR604##                                                                     ##STR605##                                                                     ##STR606##                                                                     ##STR607##                                                                     ##STR608##                                                                     ##STR609##                                                                     ##STR610##                                                                     ##STR611##                                                                     ##STR612##                                                                     ##STR613##                                                                     ##STR614##                                                                     ##STR615##                                                                     ##STR616##                                                                     ##STR617##                                                                     ##STR618##                                                                     ##STR619##                                                                     ##STR620##                                                                     ##STR621##                                                                     ##STR622##                                                                     ##STR623##                                                                     ##STR624##                                                                     ##STR625##                                                                     ##STR626##                                                                     ##STR627##                                                                     ##STR628##                                                                     ##STR629##                                                                     ##STR630##                                                                     ##STR631##                                                                     ##STR632##                                                                     ##STR633##                                                                     ##STR634##                                                                     ##STR635##                                                                     ##STR636##                                                                     ##STR637##                                                                     ##STR638##                                                                     ##STR639##                                                                     ##STR640##                                                                     ##STR641##                                                                     ##STR642##                                                                     ##STR643##                                                                     ##STR644##                                                                     ##STR645##                                                                     ##STR646##                                                                     ##STR647##                                                                     ##STR648##                                                                     ##STR649##                                                                     ##STR650##                                                                     ##STR651##                                                                     ##STR652##                                                                     ##STR653##                                                                     ##STR654##                                                                     ##STR655##                                                                     ##STR656##                                                                     ##STR657##                                                                     ##STR658##                                                                     ##STR659##                                                                     ##STR660##                                                                     ##STR661##                                                                     ##STR662##                                                                     ##STR663##                                                                     ##STR664##                                                                     ##STR665##                                                                     ##STR666##                                                                     ##STR667##                                                                     ##STR668##                                                                     ##STR669##                                                                     ##STR670##                                                                     ##STR671##                                                                     ##STR672##                                                                     ##STR673##                                                                     ##STR674##                                                                     ##STR675##                                                                     ##STR676##                                                                     ##STR677##                                                                     ##STR678##                                                                     ##STR679##                                                                     ##STR680##                                                                     ##STR681##                                                                     ##STR682##                                                                    R.sup.m represents R.sup.a1, R.sup.b1, R.sup.d1, R.sup.e1 or                   ______________________________________                                         R.sup.f1.                                                                      R.sup.m                       Gn                                               ______________________________________                                         Me                            Ga                                               Et                            Ga                                               Pr-n                          Ga                                               Pr-iso                        Gb                                               Bu-n                          Ga                                               Bu-iso                        Ga                                               Pen-n                         Gb                                               CH.sub.2 Pr-cyc               Ga                                               CH.sub.2 CH.sub.2 Pr-cyc      Gb                                               CH.sub.2 CHCH.sub.2           Ga                                               CH.sub.2 CHCHMe               Ga                                               CH.sub.2 C CH                 Ga                                               CH.sub.2 C CMe                Ga                                               CH.sub.2 CH.sub.2 OMe         Ga                                               CH.sub.2 OMe                  Ga                                               CH.sub.2 CH.sub.2 SMe         Ga                                               CH.sub.2 SMe                  Ga                                               CH.sub.2 SO.sub.2 Me          Ga                                               CH.sub.2 CH.sub.2 SO.sub.2 Me Ga                                               CH.sub.2 CF.sub.3             Ga                                               CH.sub.2 CN                   Ga                                               CH.sub.2 CH.sub.2 CN          Ga                                               CH.sub.2 NO.sub.2             Ga                                               CH.sub.2 CH.sub.2 NO.sub.2    Ga                                               CH.sub.2 COMe                 Ga                                               CH.sub.2 COEt                 Ga                                               CH.sub.2 COCHCH.sub.2         Ga                                               CH.sub.2 CHCHCOMe             Ga                                               CH.sub.2 CONMe.sub.2          Ga                                               ______________________________________                                    

                  TABLE 2A                                                         ______________________________________                                          ##STR683##                                                                     ##STR684##                                                                                     ##STR685##                                                     ##STR686##                                                                                     ##STR687##                                                     ##STR688##                                                                                     ##STR689##                                                     ##STR690##                                                                    R.sup.c1                 Gn                                                    ______________________________________                                         Me                       Ga                                                    Et                       Ga                                                    Pr-n                     Ga                                                    Pr-iso                   Ga                                                    Bu-n                     Ga                                                    Bu-iso                   Ga                                                    Bu-sec                   Ga                                                    Bu-tert                  Gb                                                    Pen-n                    Ga                                                    Hex-n                    Gb                                                    Hep-n                    Gb                                                    Pr-cyc                   Ga                                                    Hex-cyc                  Ga                                                    CH.sub.2 Pr-cyc          Ga                                                    CH.sub.2 CH.sub.2 Pr-cyc Ga                                                    CH.sub.2 Bu-cyc          Gb                                                    CH.sub.2 Pen-cyc         Gc                                                    Hexen-cyc                Gb                                                    CH.sub.2 Penten-cyc      Gb                                                    CH.sub.2 CHCH.sub.2      Ga                                                    CH.sub.2 CHCHMe          Ga                                                    CH.sub.2 CHCHEt          Ga                                                    CH.sub.2 CHCMe.sub.2     Ga                                                    CH.sub.2 CMeCH.sub.2     Ga                                                    CH.sub.2 CMeCHCHMe       Ga                                                    CH.sub.2 CH.sub.2 CHCH.sub.2                                                                            Ga                                                    CH.sub.2 CH.sub.2 CHCHMe Ga                                                    CH.sub.2 CCH             Ga                                                    CH.sub.2 CCMe            Ga                                                    CH.sub.2 CCEt            Ga                                                    CH.sub.2 CH.sub.2 CCH    Ga                                                    CH.sub.2 CH.sub.2 CCMe   Ga                                                    CHMeCCH                  Ga                                                    CHMeCCMe                 Ga                                                    CH.sub.2 OMe             Ga                                                    CH.sub.2 OEt             Ga                                                    CH.sub.2 OPr-n           Gb                                                    CH.sub.2 CH.sub.2 OMe    Ga                                                    CH.sub.2 CH.sub.2 OEt    Ga                                                    CH.sub.2 CH.sub.2 OPr-n  Gb                                                    CH.sub.2 CHMeOMe         Ga                                                    CH.sub.2 CH.sub.2 CH.sub.2 OMe                                                                          Ga                                                    CH.sub.2 CH.sub.2 CH.sub.2 OEt                                                                          Ga                                                    CH.sub.2 OCH.sub.2 CHCH.sub.2                                                                           Ga                                                    CH.sub.2 OCH.sub.2 CHCHMe                                                                               Ga                                                    CH.sub.2 CH.sub.2 OCH.sub.2 CHCH.sub.2                                                                  Ga                                                    CH.sub.2 CH.sub.2 OCH.sub.2 CHCHMe                                                                      Ga                                                    CH.sub.2 OCH.sub.2 CCH   Ga                                                    CH.sub.2 OCH.sub.2 CCMe  Ga                                                    CH.sub.2 CH.sub.2 OCH.sub.2 CCH                                                                         Ga                                                    CH.sub.2 CH.sub.2 OCH.sub.2 CCMe                                                                        Ga                                                    CH.sub.2 OCHF.sub.2      Ga                                                    CH.sub.2 OCF.sub.3       Ga                                                    CH.sub.2 CH.sub.2 OCHF.sub.2                                                                            Ga                                                    CH.sub.2 CH.sub.2 OCF.sub.3                                                                             Ga                                                    CH.sub.2 OCH.sub.2 CF.sub.3                                                                             Ga                                                    CH.sub.2 CH.sub.2 OCH.sub.2 CF.sub.3                                                                    Ga                                                    CH.sub.2 OCH.sub.2 CH.sub.2 F                                                                           Ga                                                    CH.sub.2 OCH.sub.2 CH.sub.2 Cl                                                                          Ga                                                    CH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 F                                                                  Ga                                                    CH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 Cl                                                                 Ga                                                    CH.sub.2 OCH.sub.2 CHCHCl                                                                               Gb                                                    CH.sub.2 CH.sub.2 OCH.sub.2 CHCHCl                                                                      Gb                                                    CH.sub.2 OCH.sub.2 CHCHBr                                                                               Gb                                                    CH.sub.2 CH.sub.2 OCH.sub.2 CHCHBr                                                                      Gb                                                    CH.sub.2 OCH.sub.2 CHCF.sub.2                                                                           Gb                                                    CH.sub.2 CH.sub.2 OCH.sub.2 CHCF.sub.2                                                                  Gb                                                    CH.sub.2 OCH.sub.2 CHCHCF.sub.3                                                                         Gb                                                    CH.sub.2 CH.sub.2 OCH.sub.2 CHCHCF.sub.3                                                                Gb                                                    CH.sub.2 OCH.sub.2 CCI   Gb                                                    CH.sub.2 CH.sub.2 OCH.sub.2 CCI                                                                         Gb                                                    CH.sub.2 OCH.sub.2 CCCF.sub.3                                                                           Gb                                                    CH.sub.2 CH.sub.2 OCH.sub.2 CCCF.sub.3                                                                  Gb                                                    CH.sub.2 SMe             Ga                                                    CH.sub.2 SEt             Ga                                                    CH.sub.2 SPr-n           Gb                                                    CH.sub.2 CH.sub.2 SMe    Ga                                                    CH.sub.2 CH.sub.2 SEt    Ga                                                    CH.sub.2 CH.sub.2 SPr-n  Gb                                                    CH.sub.2 SOMe            Gb                                                    CH.sub.2 SOEt            Gb                                                    CH.sub.2 CH.sub.2 SOMe   Gb                                                    CH.sub.2 CH.sub.2 SOEt   Gb                                                    CH.sub.2 SO.sub.2 Me     Ga                                                    CH.sub.2 SO.sub.2 Et     Ga                                                    CH.sub.2 SO.sub.2 Pr-n   Gb                                                    CH.sub.2 CH.sub.2 SO.sub.2 Me                                                                           Ga                                                    CH.sub.2 CH.sub.2 SO.sub.2 Et                                                                           Ga                                                    CH.sub.2 CH.sub.2 SO.sub.2 Pr-n                                                                         Gb                                                    CH.sub.2 CH.sub.2 F      Ga                                                    CH.sub.2 CHF.sub.2       Ga                                                    CH.sub.2 CF.sub.3        Ga                                                    CH.sub.2 CH.sub.2 Cl     Ga                                                    CH.sub.2 CH.sub.2 Br     Ga                                                    CH.sub.2 CH.sub.2 CF.sub.3                                                                              Ga                                                    CH.sub.2 CF.sub.2 CF.sub.3                                                                              Ga                                                    CH.sub.2 CHCHCl          Ga                                                    CH.sub.2 CHCHBr          Ga                                                    CH.sub.2 CHCF.sub.2      Ga                                                    CH.sub.2 CHCHCF.sub.3    Ga                                                    CH.sub.2 CCI             Gb                                                    CH.sub.2 CCCF.sub.3      Gb                                                    CH.sub.2 CN              Ga                                                    CH.sub.2 CH.sub.2 CN     Ga                                                    CHMeCN                   Ga                                                    CH.sub.2 CHCHCN          Ga                                                    CH(CN)CCH                Gb                                                    CH.sub.2 NO.sub.2        Ga                                                    CH.sub.2 CH.sub.2 NO.sub.2                                                                              Ga                                                    CH.sub.2 CHCHNO.sub.2    Gb                                                    CH.sub.2 CH(NO.sub.2)CHCH.sub.2                                                                         Gc                                                    CH.sub.2 CH(NO.sub.2)CCH Gc                                                    CH.sub.2 CO.sub.2 Me     Ga                                                    CH.sub.2 CO.sub.2 Et     Ga                                                    CH.sub.2 CO.sub.2 Pr-n   Gb                                                    CHMeCO.sub.2 Me          Ga                                                    CHMeCO.sub.2 Et          Ga                                                    CH.sub.2 CH.sub.2 CO.sub.2 Me                                                                           Ga                                                    CH.sub.2 CH.sub.2 CO.sub.2 Et                                                                           Ga                                                    CH.sub.2 CH.sub.2 CH.sub.2 CO.sub.2 Me                                                                  Gb                                                    CH.sub.2 CHCHCO.sub.2 Me Ga                                                    CH.sub.2 CHCHCO.sub.2 Et Ga                                                    CHMeCHCHCO.sub.2 Me      Ga                                                    CHMeCHCHCO.sub.2 Et      Ga                                                    CH.sub.2 CCCO.sub.2 Me   Ga                                                    CH.sub.2 CCCO.sub.2 Et   Ga                                                    CH.sub.2 COMe            Ga                                                    CH.sub.2 COEt            Ga                                                    CH.sub.2 COPr-n          Gb                                                    CH.sub.2 CH.sub.2 COMe   Ga                                                    CH.sub.2 CH.sub.2 COEt   Ga                                                    CH.sub.2 COCF.sub.3      Ga                                                    CH.sub.2 CH.sub.2 COCF.sub.3                                                                            Ga                                                    CH.sub.2 COCH.sub.2 CF.sub.3                                                                            Gb                                                    CH.sub.2 COCH.sub.2 F    Gb                                                    CH.sub.2 COCHCH.sub.2    Ga                                                    CH.sub.2 COCHCHMe        Ga                                                    CH.sub.2 COCH.sub.2 CHCH.sub.2                                                                          Gb                                                    CH.sub.2 CH.sub.2 COCHCH.sub.2                                                                          Gb                                                    CH.sub.2 CH.sub.2 COCHCHMe                                                                              Gb                                                    CH.sub.2 COCCH           Ga                                                    CH.sub.2 COCCMe          Ga                                                    CH.sub.2 COCH.sub.2 OMe  Ga                                                    CH.sub.2 COCH.sub.2 OEt  Ga                                                    CH.sub.2 COCH.sub.2 CH.sub.2 OMe                                                                        Ga                                                    CH.sub.2 COCH.sub.2 CH.sub.2 OEt                                                                        Ga                                                    CH.sub.2 COCH.sub.2 SMe  Ga                                                    CH.sub.2 COCH.sub.2 SEt  Ga                                                    CH.sub.2 COCH.sub.2 CH.sub.2 SMe                                                                        Ga                                                    CH.sub.2 COCH.sub.2 CH.sub.2 SEt                                                                        Ga                                                    CH.sub.2 COCH.sub.2 SOMe Gb                                                    CH.sub.2 COCH.sub.2 CH.sub.2 SOMe                                                                       Gb                                                    CH.sub.2 COCH.sub.2 SO.sub.2 Me                                                                         Ga                                                    CH.sub.2 COCH.sub.2 SO.sub.2 Et                                                                         Ga                                                    CH.sub.2 COCH.sub.2 CH.sub.2 SO.sub.2 Me                                                                Ga                                                    CH.sub.2 COCH.sub.2 CH.sub.2 SO.sub.2 Et                                                                Ga                                                    CH.sub.2 CHCHCOMe        Ga                                                    CH.sub.2 CHCHCOEt        Ga                                                    CHMeCHCHCOMe             Ga                                                    CHMeCHCHCOEt             Ga                                                    CH.sub.2 CCCOMe          Ga                                                    CH.sub.2 CCCOEt          Ga                                                    CH.sub.2 SO.sub.2 NHMe   Ga                                                    CH.sub.2 SO.sub.2 NHEt   Ga                                                    CH.sub.2 CH.sub.2 SO.sub.2 NHMe                                                                         Ga                                                    CH.sub.2 CH.sub.2 SO.sub.2 NHEt                                                                         Ga                                                    CH.sub.2 SO.sub.2 NHOMe  Ga                                                    CH.sub.2 SO.sub.2 NHOEt  Ga                                                    CH.sub.2 CH.sub.2 SO.sub.2 NHOMe                                                                        Ga                                                    CH.sub.2 CH.sub.2 SO.sub.2 NHOEt                                                                        Ga                                                    CH.sub.2 SO.sub.2 NMe.sub.2                                                                             Ga                                                    CH.sub.2 SO.sub.2 NMeEt  Ga                                                    CH.sub.2 SO.sub.2 NEt    Ga                                                    CH.sub.2 CH.sub.2 SO.sub.2 NMe.sub.2                                                                    Ga                                                    CH.sub.2 CH.sub.2 SO.sub.2 NMeEt                                                                        Ga                                                    CH.sub.2 CH.sub.2 SO.sub.2 NEt.sub.2                                                                    Ga                                                    CH.sub.2 SO.sub.2 N(OMe)Me                                                                              Ga                                                    CH.sub.2 SO.sub.2 N(OMe)Et                                                                              Ga                                                    CH.sub.2 SO.sub.2 N(OEt)Me                                                                              Ga                                                    CH.sub.2 CH.sub.2 SO.sub.2 N(OMe)Me                                                                     Ga                                                    CH.sub.2 CH.sub.2 SO.sub.2 N(OMe)Et                                                                     Ga                                                    CH.sub.2 CH.sub.2 SO.sub.2 N(OEt)Me                                                                     Ga                                                    CH.sub.2 CONHMe          Ga                                                    CH.sub.2 CONHEt          Ga                                                    CH.sub.2 CONHPr-n        Gb                                                    CH.sub.2 CH.sub.2 CONHMe Ga                                                    CH.sub.2 CH.sub.2 CONHEt Ga                                                    CH.sub.2 CH.sub.2 CONHPr-n                                                                              Gb                                                    CH.sub.2 CONMe.sub.2     Ga                                                    CH.sub.2 CONMeEt         Ga                                                    CH.sub.2 CONEt.sub.2     Ga                                                    CH.sub.2 CONHOMe         Ga                                                    CH.sub.2 CONHOEt         Ga                                                    CH.sub.2 CONHOPr-n       Gb                                                    CH.sub.2 CON(OMe)Me      Ga                                                    CH.sub.2 CON(OMe)Et      Ga                                                    CH.sub.2 CON(OEt)Me      Ga                                                    CH.sub.2 CON(OEt)Et      Ga                                                    CH.sub.2 NHMe            Ga                                                    CH.sub.2 NHEt            Ga                                                    CH.sub.2 NHPr-n          Gb                                                    CH.sub.2 CH.sub.2 NHMe   Ga                                                    CH.sub.2 CH.sub.2 NHEt   Ga                                                    CH.sub.2 CH.sub.2 NHPr-n Gb                                                    CH.sub.2 NHOMe           Ga                                                    CH.sub.2 NHOEt           Ga                                                    CH.sub.2 CH.sub.2 NHOMe  Ga                                                    CH.sub.2 CH.sub.2 NHOEt  Ga                                                    CH.sub.2 NMe.sub.2       Ga                                                    CH.sub.2 NMeEt           Ga                                                    CH.sub.2 CH.sub.2 NMe.sub.2                                                                             Ga                                                    CH.sub.2 CH.sub.2 NMeEt  Ga                                                    CH.sub.2 N(OMe)Me        Ga                                                    CH.sub.2 N(OMe)Et        Ga                                                    CH.sub.2 N(OEt)Me        Ga                                                    CH.sub.2 CH.sub.2 N(OMe)Me                                                                              Ga                                                    CH.sub.2 CH.sub.2 N(OMe)Et                                                                              Ga                                                    CH.sub.2 CH.sub.2 N(OEt)Me                                                                              Ga                                                    CH.sub.2 NMeCOMe         Ga                                                    CH.sub.2 NEtCOMe         Ga                                                    CH.sub.2 NMeCOEt         Ga                                                    CH.sub.2 CH.sub.2 NMeCOMe                                                                               Ga                                                    CH.sub.2 CH.sub.2 NEtCOMe                                                                               Ga                                                    CH.sub.2 CH.sub.2 NMeCOEt                                                                               Ga                                                    CH.sub.2 N(OMe)COMe      Ga                                                    CH.sub.2 N(OEt)COMe      Ga                                                    CH.sub.2 N(OMe)COEt      Ga                                                    CH.sub.2 CH.sub.2 N(OMe)COMe                                                                            Ga                                                    CH.sub.2 CH.sub.2 N(OEt)COMe                                                                            Ga                                                    CH.sub.2 CH.sub.2 N(OMe)COEt                                                                            Ga                                                    CH.sub.2 NMeSO.sub.2 Me  Ga                                                    CH.sub.2 NEtSO.sub.2 Me  Ga                                                    CH.sub.2 NMeSO.sub.2 Et  Ga                                                    CH.sub.2 CH.sub.2 NMeSO.sub.2 Me                                                                        Ga                                                    CH.sub.2 CH.sub.2 NEtSO.sub.2 Me                                                                        Ga                                                    CH.sub.2 CH.sub.2 NMeSO.sub.2 Et                                                                        Ga                                                    CH.sub.2 N(OMe)SO.sub.2 Me                                                                              Ga                                                    CH.sub.2 N(OEt)SO.sub.2 Me                                                                              Ga                                                    CH.sub.2 N(OMe)SO.sub.2 Et                                                                              Ga                                                    CH.sub.2 CH.sub.2 N(OMe)SO.sub.2 Me                                                                     Ga                                                    CH.sub.2 CH.sub.2 N(OEt)SO.sub.2 Me                                                                     Ga                                                    CH.sub.2 CH.sub.2 N(OMe)SO.sub.2 Et                                                                     Ga                                                    CH.sub.2 Ph              Gb                                                    CH.sub.2 CH.sub.2 Ph     Gb                                                    CH.sub.2 CH.sub.2 CH.sub.2 Ph                                                                           Gb                                                    CHMePh                   Gb                                                    CH.sub.2 CHCHPh          Ga                                                    CHMeCHCHPh               Ga                                                    CH.sub.2 CCPh            Ga                                                    CHMeCCPh                 Ga                                                    CH.sub.2 CH.sub.2 OPh    Ga                                                    CH.sub.2 OPh             Ga                                                    CH.sub.2 CH.sub.2 SPh    Ga                                                    CH.sub.2 SPh             Ga                                                    CH.sub.2 CH.sub.2 SOPh   Gb                                                    CH.sub.2 CH.sub.2 SO.sub.2 Ph                                                                           Ga                                                    CH.sub.2 OCH.sub.2 Ph    Ga                                                    CH.sub.2 CH.sub.2 OCH.sub.2 Ph                                                                          Ga                                                    CH.sub.2 SCH.sub.2 Ph    Ga                                                    CH.sub.2 CH.sub.2 SCH.sub.2 Ph                                                                          Ga                                                    CH.sub.2 SOCH.sub.2 Ph   Gb                                                    CH.sub.2 CH.sub.2 SOCH.sub.2 Ph                                                                         Gb                                                    CH.sub.2 SO.sub.2 CH.sub.2 Ph                                                                           Ga                                                    CH.sub.2 CH.sub.2 SO.sub.2 CH.sub.2 Ph                                                                  Ga                                                    CH.sub.2 COPh            Ga                                                    CH.sub.2 CH.sub.2 COPh   Ga                                                    CHMeCOPh                 Ga                                                    CH.sub.2 COCH.sub.2 Ph   Gb                                                    CHMeCOCH.sub.2 Ph        Gb                                                    CH.sub.2 CH.sub.2 CH.sub.2 F                                                                            Ga                                                    CH.sub.2 CH.sub.2 CH.sub.2 Cl                                                                           Ga                                                    CH.sub.2 C(Cl)CH.sub.2   Ga                                                    Ph                       Ga                                                    CH.sub.2 SOPh            Ga                                                    CH.sub.2 SO.sub.2 Ph     Ga                                                    CH.sub.2 C(Cl)CHCl       Ga                                                    CH.sub.2 C(F)CHCl        Ga                                                    CH.sub.2 CHCHF           Ga                                                    CH.sub.2 C(Cl)CHMe       Ga                                                    CH.sub.2 CHC(Cl)Me       Ga                                                    CH.sub.2 CFCF.sub.2      Ga                                                    CH.sub.2 CHCHCH.sub.2 F  Ga                                                    CH.sub.2 C(Br)CHMe       Ga                                                    CH.sub.2 C(Cl)CHF        Ga                                                    CH.sub.2 C(Br)CHF        Ga                                                    CH.sub.2 C(Cl)C(Cl)Me    Ga                                                    CH.sub.2 C(Br)CHBr       Ga                                                    CH.sub.2 C(Br)C(Br)Me    Ga                                                    CH.sub.2 CHC(F)CF.sub.3  Ga                                                    CH.sub.2 CHCCl.sub.2     Ga                                                    CH.sub.2 C(F)CH.sub.2    Ga                                                    CH.sub.2 CHC(F)Cl        Ga                                                    CH.sub.2 C(Cl)C(F)Cl     Ga                                                    CH.sub.2 C(F)CCl.sub.2   Ga                                                    CH.sub.2 C(Cl)CF.sub.2   Ga                                                    CH.sub.2 C(CF.sub.3)CH.sub.2                                                                            Ga                                                    CH.sub.2 CHCHI           Ga                                                    CH.sub.2 CHCBr.sub.2     Ga                                                    CH.sub.2 C(F)CHBr        Ga                                                    CH.sub.2 C(I)CH.sub.2    Ga                                                    CH.sub.2 C(Cl)CCl.sub.2  Ga                                                    CH.sub.2 C(F)C(Cl)CF.sub.3                                                                              Ga                                                    CH.sub.2 CHC(F)CF.sub.2 Cl                                                                              Ga                                                    CH.sub.2 C(Br)CH.sub.2   Ga                                                    CH.sub.2 NHSO.sub.2 Me   Gb                                                    CH.sub.2 CH.sub.2 NHSO.sub.2 Me                                                                         Gb                                                    CH.sub.2 NHCOMe          Gb                                                    CH.sub.2 CH.sub.2 NHCOMe Gb                                                    ______________________________________                                    

                  TABLE 2B                                                         ______________________________________                                          ##STR691##                                                                     ##STR692##                                                                                       ##STR693##                                                   ##STR694##                                                                                       ##STR695##                                                   ##STR696##                                                                                       ##STR697##                                                   ##STR698##                                                                                       ##STR699##                                                   ##STR700##                                                                                       ##STR701##                                                   ##STR702##                                                                                       ##STR703##                                                   ##STR704##                                                                                       ##STR705##                                                   ##STR706##                                                                                       ##STR707##                                                   ##STR708##                                                                                       ##STR709##                                                   ##STR710##                                                                                       ##STR711##                                                   ##STR712##                                                                                       ##STR713##                                                   ##STR714##                                                                                       ##STR715##                                                   ##STR716##                                                                                       ##STR717##                                                   ##STR718##                                                                                       ##STR719##                                                  R.sup.c1                 Gn                                                    ______________________________________                                         Me                       Ga                                                    Et                       Ga                                                    Pr-n                     Ga                                                    Pr-iso                   Ga                                                    Bu-n                     Ga                                                    Bu-iso                   Gb                                                    Pen-n                    Gb                                                    Hex-n                    Gb                                                    CH.sub.2 Pr-cyc          Ga                                                    CH.sub.2 CH.sub.2 Pr-cyc Ga                                                    CH.sub.2 CHCH.sub.2      Ga                                                    CH.sub.2 CHCHMe          Ga                                                    CH.sub.2 CCH             Ga                                                    CH.sub.2 CCMe            Ga                                                    CH.sub.2 OMe             Ga                                                    CH.sub.2 OEt             Ga                                                    CH.sub.2 CH.sub.2 OMe    Ga                                                    CH.sub.2 CH.sub.2 OEt    Ga                                                    CH.sub.2 OCH.sub.2 CHCH.sub.2                                                                           Ga                                                    CH.sub.2 CH.sub.2 OCH.sub.2 CHCH.sub.2                                                                  Ga                                                    CH.sub.2 OCH.sub.2 CCH   Ga                                                    CH.sub.2 CH.sub.2 OCH.sub.2 CCH                                                                         Ga                                                    CH.sub.2 OCH.sub.2 CF.sub.3                                                                             Ga                                                    CH.sub.2 CH.sub.2 OCH.sub.2 CF.sub.3                                                                    Ga                                                    CH.sub.2 SMe             Ga                                                    CH.sub.2 SEt             Ga                                                    CH.sub.2 CH.sub.2 SMe    Ga                                                    CH.sub.2 CH.sub.2 SEt    Ga                                                    CH.sub.2 SO.sub.2 Me     Ga                                                    CH.sub.2 SO.sub.2 Et     Ga                                                    CH.sub.2 CH.sub.2 SO.sub.2 Me                                                                           Ga                                                    CH.sub.2 CH.sub.2 SO.sub.2 Et                                                                           Ga                                                    CH.sub.2 CH.sub.2 F      Ga                                                    CH.sub.2 CF.sub.3        Ga                                                    CH.sub.2 CN              Ga                                                    CH.sub.2 CH.sub.2 CN     Ga                                                    CHMeCN                   Ga                                                    CH.sub.2 CHCHCN          Ga                                                    CH.sub.2 NO.sub.2        Ga                                                    CH.sub.2 CH.sub.2 NO.sub.2                                                                              Ga                                                    CH.sub.2 CO.sub.2 Me     Gb                                                    CH.sub.2 CO.sub.2 Et     Gb                                                    CHMeCO.sub.2 Me          Gb                                                    CHMeCO.sub.2 Et          Gb                                                    CH.sub.2 CH.sub.2 CO.sub.2 Me                                                                           Ga                                                    CH.sub.2 CH.sub.2 CO.sub.2 Et                                                                           Ga                                                    CH.sub.2 CHCHCO.sub.2 Me Ga                                                    CH.sub.2 CHCHCO.sub.2 Et Ga                                                    CHMeCHCHCO.sub.2 Me      Ga                                                    CH.sub.2 COMe            Ga                                                    CH.sub.2 COEt            Ga                                                    CH.sub.2 COPr-n          Gb                                                    CH.sub.2 COCF.sub.3      Ga                                                    CH.sub.2 COCHCH.sub.2    Ga                                                    CH.sub.2 COCHCHMe        Ga                                                    CH.sub.2 COCH.sub.2 OMe  Ga                                                    CH.sub.2 COCH.sub.2 OEt  Ga                                                    CH.sub.2 COCH.sub.2 CH.sub.2 OMe                                                                        Ga                                                    CH.sub.2 COCH.sub.2 CH.sub.2 OEt                                                                        Ga                                                    CH.sub.2 COCH.sub.2 SMe  Ga                                                    CH.sub.2 COCH.sub.2 CH.sub.2 SMe                                                                        Ga                                                    CH.sub.2 COCH.sub.2 SO.sub.2 Me                                                                         Ga                                                    CH.sub.2 COCH.sub.2 CH.sub.2 SO.sub.2 Me                                                                Ga                                                    CH.sub.2 CHCHCOMe        Ga                                                    CHMeCHCHCOMe             Ga                                                    CH.sub.2 SO.sub.2 NHMe   Gb                                                    CH.sub.2 CH.sub.2 SO.sub.2 NHMe                                                                         Gb                                                    CH.sub.2 SO.sub.2 NHOMe  Gb                                                    CH.sub.2 CH.sub.2 SO.sub.2 NHOMe                                                                        Gb                                                    CH.sub.2 SO.sub.2 NMe.sub.2                                                                             Ga                                                    CH.sub.2 CH.sub.2 SO.sub.2 NMe.sub.2                                                                    Ga                                                    CH.sub.2 SO.sub.2 N(OMe)Me                                                                              Ga                                                    CH.sub.2 CH.sub.2 SO.sub.2 N(OMe)Me                                                                     Ga                                                    CH.sub.2 CONHMe          Gb                                                    CH.sub.2 CH.sub.2 CONHMe Gb                                                    CH.sub.2 CONMe.sub.2     Ga                                                    CH.sub.2 CH.sub.2 CONMe.sub.2                                                                           Ga                                                    CH.sub.2 CONHOMe         Gb                                                    CH.sub.2 CH.sub.2 CONHOMe                                                                               Gb                                                    CH.sub.2 CON(OMe)Me      Ga                                                    CH.sub.2 CH.sub.2 CON(OMe)Me                                                                            Ga                                                    CH.sub.2 NHMe            Gb                                                    CH.sub.2 CH.sub.2 NHMe   Gb                                                    CH.sub.2 NHOMe           Gb                                                    CH.sub.2 CH.sub.2 NHOMe  Gb                                                    CH.sub.2 NMe.sub.2       Ga                                                    CH.sub.2 CH.sub.2 NMe.sub.2                                                                             Ga                                                    CH.sub.2 N(OMe)Me        Ga                                                    CH.sub.2 CH.sub.2 N(OMe)Me                                                                              Ga                                                    CH.sub.2 NMeCOMe         Ga                                                    CH.sub.2 CH.sub.2 NMeCOMe                                                                               Ga                                                    CH.sub.2 N(OMe)COMe      Ga                                                    CH.sub.2 CH.sub.2 N(OMe)COMe                                                                            Ga                                                    CH.sub.2 NMeSO.sub.2 Me  Ga                                                    CH.sub.2 CH.sub.2 NMeSO.sub.2 Me                                                                        Ga                                                    CH.sub.2 N(OMe)SO.sub.2 Me                                                                              Ga                                                    CH.sub.2 CH.sub.2 N(OMe)SO.sub.2 Me                                                                     Ga                                                    CH.sub.2 Ph              Gb                                                    CH.sub.2 CH.sub.2 Ph     Gb                                                    CH.sub.2 CH.sub.2 CH.sub.2 Ph                                                                           Gb                                                    CHMePh                   Gb                                                    CH.sub.2 CHCHPh          Gb                                                    CHMeCHCHPh               Gb                                                    CH.sub.2 CH.sub.2 OPh    Gb                                                    CH.sub.2 OPh             Gb                                                    CH.sub.2 CH.sub.2 SPh    Gb                                                    CH.sub.2 SPh             Gb                                                    CH.sub.2 CH.sub.2 SO.sub.2 Ph                                                                           Gb                                                    CH.sub.2 COPh            Gb                                                    CH.sub.2 CH.sub.2 COPh   Gb                                                    CH.sub.2 COCH.sub.2 Ph   Gb                                                    CH.sub.2 CH.sub.2 COCH.sub.2 Ph                                                                         Gb                                                    Ph                       Ga                                                    ______________________________________                                    

                  TABLE 2C                                                         ______________________________________                                          ##STR720##                                                                     ##STR721##                                                                     ##STR722##                                                                     ##STR723##                                                                     ##STR724##                                                                     ##STR725##                                                                     ##STR726##                                                                     ##STR727##                                                                     ##STR728##                                                                     ##STR729##                                                                     ##STR730##                                                                     ##STR731##                                                                     ##STR732##                                                                     ##STR733##                                                                     ##STR734##                                                                     ##STR735##                                                                     ##STR736##                                                                     ##STR737##                                                                     ##STR738##                                                                     ##STR739##                                                                     ##STR740##                                                                     ##STR741##                                                                     ##STR742##                                                                     ##STR743##                                                                     ##STR744##                                                                     ##STR745##                                                                     ##STR746##                                                                     ##STR747##                                                                     ##STR748##                                                                     ##STR749##                                                                     ##STR750##                                                                     ##STR751##                                                                     ##STR752##                                                                     ##STR753##                                                                     ##STR754##                                                                     ##STR755##                                                                     ##STR756##                                                                     ##STR757##                                                                     ##STR758##                                                                     ##STR759##                                                                     ##STR760##                                                                     ##STR761##                                                                     ##STR762##                                                                     ##STR763##                                                                     ##STR764##                                                                     ##STR765##                                                                     ##STR766##                                                                     ##STR767##                                                                     ##STR768##                                                                     ##STR769##                                                                     ##STR770##                                                                     ##STR771##                                                                     ##STR772##                                                                     ##STR773##                                                                     ##STR774##                                                                     ##STR775##                                                                     ##STR776##                                                                     ##STR777##                                                                     ##STR778##                                                                     ##STR779##                                                                     ##STR780##                                                                     ##STR781##                                                                     ##STR782##                                                                     ##STR783##                                                                     ##STR784##                                                                     ##STR785##                                                                     ##STR786##                                                                     ##STR787##                                                                     ##STR788##                                                                     ##STR789##                                                                     ##STR790##                                                                     ##STR791##                                                                     ##STR792##                                                                     ##STR793##                                                                     ##STR794##                                                                     ##STR795##                                                                     ##STR796##                                                                     ##STR797##                                                                     ##STR798##                                                                     ##STR799##                                                                     ##STR800##                                                                     ##STR801##                                                                     ##STR802##                                                                     ##STR803##                                                                     ##STR804##                                                                     ##STR805##                                                                     ##STR806##                                                                     ##STR807##                                                                     ##STR808##                                                                     ##STR809##                                                                     ##STR810##                                                                     ##STR811##                                                                     ##STR812##                                                                     ##STR813##                                                                     ##STR814##                                                                     ##STR815##                                                                    R.sup.c1           Gn                                                          ______________________________________                                         Me                 Ga                                                          Et                 Ga                                                          Pr-n               Ga                                                          Pro-iso            Gb                                                          Bu-n               Ga                                                          Bu-iso             Ga                                                          Pen-n              Gb                                                          CH.sub.2 Pr-cyc    Ga                                                          CH.sub.2 CH.sub.2 Pr-cyc                                                                          Gb                                                          CH.sub.2 CHCH.sub.2                                                                               Ga                                                          CH.sub.2 CHCHMe    Ga                                                          CH.sub.2 CCH       Ga                                                          CH.sub.2 CCMe      Ga                                                          CH.sub.2 CH.sub.2 OMe                                                                             Ga                                                          CH.sub.2 OMe       Ga                                                          CH.sub.2 CH.sub.2 SMe                                                                             Ga                                                          CH.sub.2 SMe       Ga                                                          CH.sub.2 SO.sub.2 Me                                                                              Ga                                                          CH.sub.2 CH.sub.2 SO.sub.2 Me                                                                     Ga                                                          CH.sub.2 CF.sub.3  Ga                                                          CH.sub.2 CN        Ga                                                          CH.sub.2 CH.sub.2 CN                                                                              Ga                                                          CH.sub.2 NO.sub.2  Ga                                                          CH.sub.2 CH.sub.2 NO.sub.2                                                                        Ga                                                          CH.sub.2 COMe      Ga                                                          CH.sub.2 COEt      Ga                                                          CH.sub.2 COCHCH.sub.2                                                                             Ga                                                          CH.sub.2 CHCHCOMe  Ga                                                          CH.sub.2 CONMe.sub.2                                                                              Ga                                                          Ph                 Ga                                                          ______________________________________                                    

                  TABLE 3                                                          ______________________________________                                          ##STR816##                                                                     ##STR817##                                                                     ##STR818##                                                                     ##STR819##                                                                     ##STR820##                                                                     ##STR821##                                                                     ##STR822##                                                                     ##STR823##                                                                     ##STR824##                                                                     ##STR825##                                                                     ##STR826##                                                                     ##STR827##                                                                     ##STR828##                                                                     ##STR829##                                                                     ##STR830##                                                                     ##STR831##                                                                     ##STR832##                                                                     ##STR833##                                                                     ##STR834##                                                                     ##STR835##                                                                     ##STR836##                                                                     ##STR837##                                                                     ##STR838##                                                                     ##STR839##                                                                     ##STR840##                                                                     ##STR841##                                                                     ##STR842##                                                                     ##STR843##                                                                     ##STR844##                                                                     ##STR845##                                                                     ##STR846##                                                                     ##STR847##                                                                     ##STR848##                                                                     ##STR849##                                                                     ##STR850##                                                                     ##STR851##                                                                     ##STR852##                                                                     ##STR853##                                                                     ##STR854##                                                                     ##STR855##                                                                     ##STR856##                                                                     ##STR857##                                                                     ##STR858##                                                                     ##STR859##                                                                     ##STR860##                                                                     ##STR861##                                                                     ##STR862##                                                                     ##STR863##                                                                     ##STR864##                                                                     ##STR865##                                                                     ##STR866##                                                                     ##STR867##                                                                     ##STR868##                                                                     ##STR869##                                                                     ##STR870##                                                                     ##STR871##                                                                     ##STR872##                                                                     ##STR873##                                                                     ##STR874##                                                                     ##STR875##                                                                     ##STR876##                                                                    R.sup.n          Gn                                                            ______________________________________                                         Me               Ga                                                            Et               Ga                                                            Pr-n             Ga                                                            Pr-iso           Gb                                                            Bu-n             Gb                                                            Pen-n            Gb                                                            Hex-n            Gb                                                            CH.sub.2 CHCH.sub.2                                                                             Ga                                                            CH.sub.2 CHCHMe  Ga                                                            CH.sub.2 CHCMe.sub.2                                                                            Gb                                                            CHMeCHCH.sub.2   Gb                                                            CH.sub.2 CCH     Ga                                                            CH.sub.2 CCMe    Ga                                                            CHMeCCH          Gb                                                            CH.sub.2 SMe     Ga                                                            CH.sub.2 SEt     Ga                                                            CH.sub.2 SPr-n   Gb                                                            CH.sub.2 CH.sub.2 SMe                                                                           Ga                                                            CH.sub.2 CH.sub.2 SEt                                                                           Ga                                                            CH.sub.2 SOMe    Gb                                                            CH.sub.2 SOEt    Gb                                                            CH.sub.2 CH.sub.2 SOMe                                                                          Gb                                                            CH.sub.2 CH.sub.2 SOEt                                                                          Gb                                                            CH.sub.2 SO.sub.2 Me                                                                            Ga                                                            CH.sub.2 SO.sub.2 Et                                                                            Ga                                                            CH.sub.2 SO.sub.2 Pr-n                                                                          Gb                                                            CH.sub.2 CH.sub.2 SO.sub.2 Me                                                                   Ga                                                            CH.sub.2 CH.sub.2 SO.sub.2 Et                                                                   Ga                                                            CH.sub.2 OMe     Ga                                                            CH.sub.2 OEt     Ga                                                            CH.sub.2 OPr-n   Gb                                                            CH.sub.2 CH.sub.2 OMe                                                                           Ga                                                            CH.sub.2 CH.sub.2 OEt                                                                           Ga                                                            CH.sub.2 CH.sub.2 OPr-n                                                                         Gb                                                            CH.sub.2 CO.sub.2 Me                                                                            Ga                                                            CH.sub.2 CO.sub.2 Et                                                                            Ga                                                            CHMeCO.sub.2 Me  Ga                                                            CHMeCO.sub.2 Et  Ga                                                            CH.sub.2 COMe    Ga                                                            CH.sub.2 COEt    Ga                                                            CH.sub.2 COPr-n  Gb                                                            CH.sub.2 CH.sub.2 COMe                                                                          Ga                                                            CH.sub.2 CH.sub.2 COEt                                                                          Ga                                                            CH.sub.2 CN      Ga                                                            CH.sub.2 CH.sub.2 CN                                                                            Ga                                                            CH.sub.2 CH.sub.2 CH.sub.2 CN                                                                   Ga                                                            Ph               Ga                                                            CH.sub.2 Ph      Ga                                                            CH.sub.2 CH.sub.2 Ph                                                                            Ga                                                            CHMePh           Ga                                                            ______________________________________                                          R.sup.n represents R.sup.d6 or R.sup.f2.                                 

                  TABLE 4A                                                         ______________________________________                                          ##STR877##                                                                     ##STR878##                                                                                       ##STR879##                                                   ##STR880##                                                                                       ##STR881##                                                   ##STR882##                                                                                       ##STR883##                                                   ##STR884##                                                                                       ##STR885##                                                   ##STR886##                                                                                       ##STR887##                                                   ##STR888##                                                                                       ##STR889##                                                   ##STR890##                                                                                       ##STR891##                                                   ##STR892##                                                                                       ##STR893##                                                   ##STR894##                                                                                       ##STR895##                                                   ##STR896##                                                                                       ##STR897##                                                   ##STR898##                                                                                       ##STR899##                                                   ##STR900##                                                                                       ##STR901##                                                   ##STR902##                                                                                       ##STR903##                                                   ##STR904##                                                                                       ##STR905##                                                   ##STR906##                                                                                       ##STR907##                                                   ##STR908##                                                                                       ##STR909##                                                   ##STR910##                                                                                       ##STR911##                                                   ##STR912##                                                                                       ##STR913##                                                   ##STR914##                                                                    R.sup.g1                 Gn                                                    ______________________________________                                         Me                       Ga                                                    Et                       Ga                                                    Pr-n                     Ga                                                    Pr-iso                   Ga                                                    Bu-n                     Ga                                                    Bu-iso                   Ga                                                    Bu-sec                   Gb                                                    Bu-tert                  Gb                                                    Pen-n                    Ga                                                    Hex-n                    Gb                                                    Hep-n                    Gb                                                    Pr-cyc                   Ga                                                    Hex-cyc                  Ga                                                    CH.sub.2 Pr-cyc          Ga                                                    CH.sub.2 CH.sub.2 Pr-cyc Ga                                                    CH.sub.2 Bu-cyc          Gb                                                    CH.sub.2 Pen-cyc         Gc                                                    Hexen-cyc                Gb                                                    CH.sub.2 Penten-cyc      Gb                                                    CH.sub.2 CHCH.sub.2      Ga                                                    CH.sub.2 CHCHMe          Ga                                                    CH.sub.2 CHCHEt          Ga                                                    CH.sub.2 CHCMe.sub.2     Gb                                                    CH.sub.2 CMeCH.sub.2     Gb                                                    CH.sub.2 CMeCHCHMe       Gc                                                    CH.sub.2 CH.sub.2 CHCH.sub.2                                                                            Gb                                                    CH.sub.2 CH.sub.2 CHCHMe Gb                                                    CH.sub.2 CCH             Ga                                                    CH.sub.2 CCMe            Ga                                                    CH.sub.2 CCEt            Ga                                                    CH.sub.2 CH.sub.2 CCH    Gb                                                    CH.sub.2 CH.sub.2 CCMe   Gb                                                    CHMeCCH                  Gb                                                    CHMeCCMe                 Gc                                                    CH.sub.2 OMe             Ga                                                    CH.sub.2 OEt             Ga                                                    CH.sub.2 OPr-n           Gb                                                    CH.sub.2 CH.sub.2 OMe    Ga                                                    CH.sub.2 CH.sub.2 OEt    Ga                                                    CH.sub.2 CH.sub.2 OPr-n  Gb                                                    CH.sub.2 CHMeOMe         Gb                                                    CH.sub.2 CH.sub.2 CH.sub.2 OMe                                                                          Ga                                                    CH.sub.2 CH.sub.2 CH.sub.2 OEt                                                                          Ga                                                    CH.sub.2 OCH.sub.2 CHCH.sub.2                                                                           Ga                                                    CH.sub.2 OCH.sub.2 CHCHMe                                                                               Ga                                                    CH.sub.2 CH.sub.2 OCH.sub.2 CHCH.sub.2                                                                  Ga                                                    CH.sub.2 CH.sub.2 OCH.sub.2 CHCHMe                                                                      Ga                                                    CH.sub.2 OCH.sub.2 CCH   Ga                                                    CH.sub.2 OCH.sub.2 CCMe  Ga                                                    CH.sub.2 CH.sub.2 OCH.sub.2 CCH                                                                         Ga                                                    CH.sub.2 CH.sub.2 OCH.sub.2 CCMe                                                                        Ga                                                    CH.sub.2 OCHF.sub.2      Ga                                                    CH.sub.2 OCF.sub.3       Ga                                                    CH.sub.2 CH.sub.2 OCHF.sub.2                                                                            Ga                                                    CH.sub.2 CH.sub.2 OCF.sub.3                                                                             Ga                                                    CH.sub.2 OCH.sub.2 CF.sub.3                                                                             Ga                                                    CH.sub.2 CH.sub.2 OCH.sub.2 CF.sub.3                                                                    Ga                                                    CH.sub.2 OCH.sub.2 CH.sub.2 F                                                                           Ga                                                    CH.sub.2 OCH.sub.2 CH.sub.2 Cl                                                                          Ga                                                    CH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 F                                                                  Ga                                                    CH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 Cl                                                                 Ga                                                    CH.sub.2 OCH.sub.2 CHCHCl                                                                               Gb                                                    CH.sub.2 CH.sub.2 OCH.sub.2 CHCHCl                                                                      Gb                                                    CH.sub.2 OCH.sub.2 CHCHBr                                                                               Gb                                                    CH.sub.2 CH.sub.2 OCH.sub.2 CHCHBr                                                                      Gb                                                    CH.sub.2 OCH.sub.2 CHCF.sub.2                                                                           Gb                                                    CH.sub.2 CH.sub.2 OCH.sub.2 CHCF.sub.2                                                                  Gb                                                    CH.sub.2 OCH.sub.2 CHCHCF.sub.3                                                                         Gb                                                    CH.sub.2 CH.sub.2 OCH.sub.2 CHCHCF.sub.3                                                                Gb                                                    CH.sub.2 OCH.sub.2 CCI   Gb                                                    CH.sub.2 CH.sub.2 OCH.sub.2 CCI                                                                         Gb                                                    CH.sub.2 OCH.sub.2 CCCF.sub.3                                                                           Gb                                                    CH.sub.2 CH.sub.2 OCH.sub.2 CCCF.sub.3                                                                  Gb                                                    CH.sub.2 SMe             Ga                                                    CH.sub.2 SEt             Ga                                                    CH.sub.2 SPr-n           Gb                                                    CH.sub.2 CH.sub.2 SMe    Ga                                                    CH.sub.2 CH.sub.2 SEt    Ga                                                    CH.sub.2 CH.sub.2 SPr-n  Gb                                                    CH.sub.2 SOMe            Gb                                                    CH.sub.2 SOEt            Gb                                                    CH.sub.2 CH.sub.2 SOMe   Gb                                                    CH.sub.2 CH.sub.2 SOEt   Gb                                                    CH.sub.2 SO.sub.2 Me     Ga                                                    CH.sub.2 SO.sub.2 Et     Ga                                                    CH.sub.2 SO.sub.2 Pr-n   Gb                                                    CH.sub.2 CH.sub.2 SO.sub.2 Me                                                                           Ga                                                    CH.sub.2 CH.sub.2 SO.sub.2 Et                                                                           Ga                                                    CH.sub.2 CH.sub.2 SO.sub.2 Pr-n                                                                         Gb                                                    CH.sub.2 CH.sub.2 F      Ga                                                    CH.sub.2 CHF.sub.2       Ga                                                    CH.sub.2 CF.sub.3        Ga                                                    CH.sub.2 CH.sub.2 Cl     Ga                                                    CH.sub.2 CH.sub.2 Br     Ga                                                    CH.sub.2 CH.sub.2 CF.sub.3                                                                              Ga                                                    CH.sub.2 CF.sub.2 CF.sub.3                                                                              Ga                                                    CH.sub.2 CHCHCl          Gb                                                    CH.sub.2 CHCHBr          Gb                                                    CH.sub.2 CHCF.sub.2      Gb                                                    CH.sub.2 CHCHCF.sub.3    Gb                                                    CH.sub.2 CCI             Gb                                                    CH.sub.2 CCCF.sub.3      Gb                                                    CH.sub.2 CN              Ga                                                    CH.sub.2 CH.sub.2 CN     Ga                                                    CHMeCN                   Ga                                                    CH.sub.2 CHCHCN          Ga                                                    CH(CN)CCH                Gb                                                    CH.sub.2 NO.sub.2        Ga                                                    CH.sub.2 CH.sub.2 NO.sub.2                                                                              Ga                                                    CH.sub.2 CHCHNO.sub.2    Gb                                                    CH.sub.2 CH(NO.sub.2)CHCH.sub.2                                                                         Gc                                                    CH.sub.2 CH(NO.sub.2)CCH Gc                                                    CH.sub.2 CO.sub.2 Me     Gb                                                    CH.sub.2 CO.sub.2 Et     Gb                                                    CH.sub.2 CO.sub.2 Pr-n   Gb                                                    CHMeCO.sub.2 Me          Gb                                                    CHMeCO.sub.2 Et          Gb                                                    CH.sub.2 CH.sub.2 CO.sub.2 Me                                                                           Ga                                                    CH.sub.2 CH.sub.2 CO.sub.2 Et                                                                           Ga                                                    CH.sub.2 CH.sub.2 CH.sub.2 CO.sub.2 Me                                                                  Gb                                                    CH.sub.2 CHCHCO.sub.2 Me Ga                                                    CH.sub.2 CHCHCO.sub.2 Et Ga                                                    CHMeCHCHCO.sub.2 Me      Ga                                                    CHMeCHCHCO.sub.2 Et      Ga                                                    CH.sub.2 CCCO.sub.2 Me   Ga                                                    CH.sub.2 CCCO.sub.2 Et   Ga                                                    CH.sub.2 COMe            Ga                                                    CH.sub.2 COEt            Ga                                                    CH.sub.2 COPr-n          Gb                                                    CH.sub.2 CH.sub.2 COMe   Ga                                                    CH.sub.2 CH.sub.2 COEt   Ga                                                    CH.sub.2 COCF.sub.3      Ga                                                    CH.sub.2 CH.sub.2 COCF.sub.3                                                                            Ga                                                    CH.sub.2 COCH.sub.2 CF.sub.3                                                                            Gb                                                    CH.sub.2 COCH.sub.2 F    Gb                                                    CH.sub.2 COCHCH.sub.2    Ga                                                    CH.sub.2 COCHCHMe        Ga                                                    CH.sub.2 COCH.sub.2 CHCH.sub.2                                                                          Gb                                                    CH.sub.2 CH.sub.2 COCHCH.sub.2                                                                          Gb                                                    CH.sub.2 CH.sub.2 COCHCHMe                                                                              Gb                                                    CH.sub.2 COCCH           Ga                                                    CH.sub.2 COCCMe          Ga                                                    CH.sub.2 COCH.sub.2 OMe  Ga                                                    CH.sub.2 COCH.sub.2 OEt  Ga                                                    CH.sub.2 COCH.sub.2 CH.sub.2 OMe                                                                        Ga                                                    CH.sub.2 COCH.sub.2 CH.sub.2 OEt                                                                        Ga                                                    CH.sub.2 COCH.sub.2 SMe  Ga                                                    CH.sub.2 COCH.sub.2 SEt  Ga                                                    CH.sub.2 COCH.sub.2 CH.sub.2 SMe                                                                        Ga                                                    CH.sub.2 COCH.sub.2 CH.sub.2 SEt                                                                        Ga                                                    CH.sub.2 COCH.sub.2 SOMe Gb                                                    CH.sub.2 COCH.sub.2 CH.sub.2 SOMe                                                                       Gb                                                    CH.sub.2 COCH.sub.2 SO.sub.2 Me                                                                         Ga                                                    CH.sub.2 COCH.sub.2 SO.sub.2 Et                                                                         Ga                                                    CH.sub.2 COCH.sub.2 CH.sub.2 SO.sub.2 Me                                                                Ga                                                    CH.sub.2 COCH.sub.2 CH.sub.2 SO.sub.2 Et                                                                Ga                                                    CH.sub.2 CHCHCOMe        Ga                                                    CH.sub.2 CHCHCOEt        Ga                                                    CHMeCHCHCOMe             Ga                                                    CHMeCHCHCOEt             Ga                                                    CH.sub.2 CCCOMe          Ga                                                    CH.sub.2 CCCOEt          Ga                                                    CH.sub.2 SO.sub.2 NHMe   Ga                                                    CH.sub.2 SO.sub.2 NHEt   Ga                                                    CH.sub.2 CH.sub.2 SO.sub.2 NHMe                                                                         Ga                                                    CH.sub.2 CH.sub.2 SO.sub.2 NHEt                                                                         Ga                                                    CH.sub.2 SO.sub.2 NHOMe  Ga                                                    CH.sub.2 SO.sub.2 NHOEt  Ga                                                    CH.sub.2 CH.sub.2 SO.sub.2 NHOMe                                                                        Ga                                                    CH.sub.2 CH.sub.2 SO.sub.2 NHOEt                                                                        Ga                                                    CH.sub.2 SO.sub.2 NMe.sub.2                                                                             Ga                                                    CH.sub.2 SO.sub.2 NMeEt  Ga                                                    CH.sub.2 SO.sub.2 NEt.sub.2                                                                             Ga                                                    CH.sub.2 CH.sub.2 SO.sub.2 NMe.sub.2                                                                    Ga                                                    CH.sub.2 CH.sub.2 SO.sub.2 NMeEt                                                                        Ga                                                    CH.sub.2 CH.sub.2 SO.sub.2 NEt.sub.2                                                                    Ga                                                    CH.sub.2 SO.sub.2 N(OMe)Me                                                                              Ga                                                    CH.sub.2 SO.sub.2 N(OMe)Et                                                                              Ga                                                    CH.sub.2 SO.sub.2 N(OEt)Me                                                                              Ga                                                    CH.sub.2 CH.sub.2 SO.sub.2 N(OMe)Me                                                                     Ga                                                    CH.sub.2 CH.sub.2 SO.sub.2 N(OMe)Et                                                                     Ga                                                    CH.sub.2 CH.sub.2 SO.sub.2 N(OEt)Me                                                                     Ga                                                    CH.sub.2 CONHMe          Ga                                                    CH.sub.2 CONHEt          Ga                                                    CH.sub.2 CONHPr-n        Gb                                                    CH.sub.2 CH.sub.2 CONHMe Ga                                                    CH.sub.2 CH.sub.2 CONHEt Ga                                                    CH.sub.2 CH.sub.2 CONHPr-n                                                                              Gb                                                    CH.sub.2 CONMe.sub.2     Ga                                                    CH.sub.2 CONMeEt         Ga                                                    CH.sub.2 CONEt.sub.2     Ga                                                    CH.sub.2 CONHOMe         Ga                                                    CH.sub.2 CONHOEt         Ga                                                    CH.sub.2 CONHOPr-n       Gb                                                    CH.sub.2 CON(OMe)Me      Ga                                                    CH.sub.2 CON(OMe)Et      Ga                                                    CH.sub.2 CON(OEt)Me      Ga                                                    CH.sub.2 CON(OEt)Et      Ga                                                    CH.sub.2 NHMe            Ga                                                    CH.sub.2 NHEt            Ga                                                    CH.sub.2 NHPr-n          Gb                                                    CH.sub.2 CH.sub.2 NHMe   Ga                                                    CH.sub.2 CH.sub.2 NHEt   Ga                                                    CH.sub.2 CH.sub.2 NHPr-n Gb                                                    CH.sub.2 NHOMe           Ga                                                    CH.sub.2 NHOEt           Ga                                                    CH.sub.2 CH.sub.2 NHOMe  Ga                                                    CH.sub.2 CH.sub.2 NHOEt  Ga                                                    CH.sub.2 NMe.sub.2       Ga                                                    CH.sub.2 NMeEt           Ga                                                    CH.sub.2 CH.sub.2 NMe.sub.2                                                                             Ga                                                    CH.sub.2 CH.sub.2 NMeEt  Ga                                                    CH.sub.2 N(OMe)Me        Ga                                                    CH.sub.2 N(OMe)Et        Ga                                                    CH.sub.2 N(OEt)Me        Ga                                                    CH.sub.2 CH.sub.2 N(OMe)Me                                                                              Ga                                                    CH.sub.2 CH.sub.2 N(OMe)Et                                                                              Ga                                                    CH.sub.2 CH.sub.2 N(OEt)Me                                                                              Ga                                                    CH.sub.2 NMeCOMe         Ga                                                    CH.sub.2 NEtCOMe         Ga                                                    CH.sub.2 NMeCOEt         Ga                                                    CH.sub.2 CH.sub.2 NMeCOMe                                                                               Ga                                                    CH.sub.2 CH.sub.2 NEtCOMe                                                                               Ga                                                    CH.sub.2 CH.sub.2 NMeCOEt                                                                               Ga                                                    CH.sub.2 N(OMe)COMe      Ga                                                    CH.sub.2 N(OEt)COMe      Ga                                                    CH.sub.2 N(OMe)COEt      Ga                                                    CH.sub.2 CH.sub.2 N(OMe)COMe                                                                            Ga                                                    CH.sub.2 CH.sub.2 N(OEt)COMe                                                                            Ga                                                    CH.sub.2 CH.sub.2 N(OMe)COEt                                                                            Ga                                                    CH.sub.2 NMeSO.sub.2 Me  Ga                                                    CH.sub.2 NEtSO.sub.2 Me  Ga                                                    CH.sub.2 NMeSO.sub.2 Et  Ga                                                    CH.sub.2 CH.sub.2 NMeSO.sub.2 Me                                                                        Ga                                                    CH.sub.2 CH.sub.2 NEtSO.sub.2 Me                                                                        Ga                                                    CH.sub.2 CH.sub.2 NMeSO.sub.2 Et                                                                        Ga                                                    CH.sub.2 N(OMe)SO.sub.2 Me                                                                              Ga                                                    CH.sub.2 N(OEt)SO.sub.2 Me                                                                              Ga                                                    CH.sub.2 N(OMe)SO.sub.2 Et                                                                              Ga                                                    CH.sub.2 CH.sub.2 N(OMe)SO.sub.2 Me                                                                     Ga                                                    CH.sub.2 CH.sub.2 N(OEt)SO.sub.2 Me                                                                     Ga                                                    CH.sub.2 CH.sub.2 N(OMe)SO.sub.2 Et                                                                     Ga                                                    CH.sub.2 Ph              Gb                                                    CH.sub.2 CH.sub.2 Ph     Gb                                                    CH.sub.2 CH.sub.2 CH.sub.2 Ph                                                                           Gb                                                    CHMePh                   Gb                                                    CH.sub.2 CHCHPh          Ga                                                    CHMeCHCHPh               Ga                                                    CH.sub.2 CCPh            Ga                                                    CHMeCCPh                 Ga                                                    CH.sub.2 CH.sub.2 OPh    Ga                                                    CH.sub.2 OPh             Ga                                                    CH.sub.2 CH.sub.2 SPh    Ga                                                    CH.sub.2 SPh             Ga                                                    CH.sub.2 CH.sub.2 SOPh   Gb                                                    CH.sub.2 CH.sub.2 SO.sub.2 Ph                                                                           Ga                                                    CH.sub.2 OCH.sub.2 Ph    Ga                                                    CH.sub.2 CH.sub.2 OCH.sub.2 Ph                                                                          Ga                                                    CH.sub.2 SCH.sub.2 Ph    Ga                                                    CH.sub.2 CH.sub.2 SCH.sub.2 Ph                                                                          Ga                                                    CH.sub.2 SOCH.sub.2 Ph   Gb                                                    CH.sub.2 CH.sub.2 SOCH.sub.2 Ph                                                                         Gb                                                    CH.sub.2 SO.sub.2 CH.sub.2 Ph                                                                           Ga                                                    CH.sub.2 CH.sub.2 SO.sub.2 CH.sub.2 Ph                                                                  Ga                                                    CH.sub.2 COPh            Ga                                                    CH.sub.2 CH.sub.2 COPh   Ga                                                    CHMeCOPh                 Ga                                                    CH.sub.2 COCH.sub.2 Ph   Gb                                                    CHMeCOCH.sub.2 Ph        Gb                                                    CH.sub.2 CH.sub.2 CH.sub.2 F                                                                            Ga                                                    CH.sub.2 CH.sub.2 CH.sub.2 Cl                                                                           Ga                                                    ______________________________________                                    

                  TABLE 4B                                                         ______________________________________                                          ##STR915##                                                                     ##STR916##                                                                                       ##STR917##                                                   ##STR918##                                                                                       ##STR919##                                                   ##STR920##                                                                                       ##STR921##                                                   ##STR922##                                                                                       ##STR923##                                                   ##STR924##                                                                                       ##STR925##                                                   ##STR926##                                                                                       ##STR927##                                                   ##STR928##                                                                                       ##STR929##                                                   ##STR930##                                                                                       ##STR931##                                                   ##STR932##                                                                                       ##STR933##                                                   ##STR934##                                                                                       ##STR935##                                                   ##STR936##                                                                                       ##STR937##                                                   ##STR938##                                                                                       ##STR939##                                                   ##STR940##                                                                                       ##STR941##                                                   ##STR942##                                                                                       ##STR943##                                                   ##STR944##                                                                                       ##STR945##                                                   ##STR946##                                                                    R.sup.g1                 Gn                                                    ______________________________________                                         Me                       Ga                                                    Et                       Ga                                                    Pr-n                     Ga                                                    Pr-iso                   Ga                                                    Bu-n                     Ga                                                    Bu-iso                   Gb                                                    Pen-n                    Gb                                                    Hex-n                    Gb                                                    CH.sub.2 Pr-cyc          Ga                                                    CH.sub.2 CH.sub.2 Pr-cyc Ga                                                    CH.sub.2 CHCH.sub.2      Ga                                                    CH.sub.2 CHCHMe          Ga                                                    CH.sub.2 CCH             Ga                                                    CH.sub.2 CCMe            Ga                                                    CH.sub.2 OMe             Ga                                                    CH.sub.2 OEt             Ga                                                    CH.sub.2 CH.sub.2 OMe    Ga                                                    CH.sub.2 CH.sub.2 OEt    Ga                                                    CH.sub.2 OCH.sub.2 CHCH.sub.2                                                                           Ga                                                    CH.sub.2 CH.sub.2 OCH.sub.2 CHCH.sub.2                                                                  Ga                                                    CH.sub.2 OCH.sub.2 CCH   Ga                                                    CH.sub.2 CH.sub.2 OCH.sub.2 CCH                                                                         Ga                                                    CH.sub.2 OCH.sub.2 CF.sub.3                                                                             Ga                                                    CH.sub.2 CH.sub.2 OCH.sub.2 CF.sub.3                                                                    Ga                                                    CH.sub.2 SMe             Ga                                                    CH.sub.2 SEt             Ga                                                    CH.sub.2 CH.sub.2 SMe    Ga                                                    CH.sub.2 CH.sub.2 SEt    Ga                                                    CH.sub.2 SO.sub.2 Me     Ga                                                    CH.sub.2 SO.sub.2 Et     Ga                                                    CH.sub.2 CH.sub.2 SO.sub.2 Me                                                                           Ga                                                    CH.sub.2 CH.sub.2 SO.sub.2 Et                                                                           Ga                                                    CH.sub.2 CH.sub.2 F      Ga                                                    CH.sub.2 CF.sub.3        Ga                                                    CH.sub.2 CN              Ga                                                    CH.sub.2 CH.sub.2 CN     Ga                                                    CHMeCN                   Ga                                                    CH.sub.2 CHCHCN          Ga                                                    CH.sub.2 NO.sub.2        Ga                                                    CH.sub.2 CH.sub.2 NO.sub.2                                                                              Ga                                                    CH.sub.2 CO.sub.2 Me     Gb                                                    CH.sub.2 CO.sub.2 Et     Gb                                                    CHMeCO.sub.2 Me          Gb                                                    CHMeCO.sub.2 Et          Gb                                                    CH.sub.2 CH.sub.2 CO.sub.2 Me                                                                           Ga                                                    CH.sub.2 CH.sub.2 CO.sub.2 Et                                                                           Ga                                                    CH.sub.2 CHCHCO.sub.2 Me Ga                                                    CH.sub.2 CHCHCO.sub.2 Et Ga                                                    CHMeCHCHCO.sub.2 Me      Ga                                                    CH.sub.2 COMe            Ga                                                    CH.sub.2 COEt            Ga                                                    CH.sub.2 COPr-n          Gb                                                    CH.sub.2 COCF.sub.3      Ga                                                    CH.sub.2 COCHCH.sub.2    Ga                                                    CH.sub.2 COCHCHMe        Ga                                                    CH.sub.2 COCH.sub.2 OMe  Ga                                                    CH.sub.2 COCH.sub.2 OEt  Ga                                                    CH.sub.2 COCH.sub.2 CH.sub.2 OMe                                                                        Ga                                                    CH.sub.2 COCH.sub.2 CH.sub.2 OEt                                                                        Ga                                                    CH.sub.2 COCH.sub.2 SMe  Ga                                                    CH.sub.2 COCH.sub.2 CH.sub.2 SMe                                                                        Ga                                                    CH.sub.2 COCH.sub.2 SO.sub.2 Me                                                                         Ga                                                    CH.sub.2 COCH.sub.2 CH.sub.2 SO.sub.2 Me                                                                Ga                                                    CH.sub.2 CHCHCOMe        Ga                                                    CHMeCHCHCOMe             Ga                                                    CH.sub.2 SO.sub.2 NHMe   Gb                                                    CH.sub.2 CH.sub.2 SO.sub.2 NHMe                                                                         Gb                                                    CH.sub.2 SO.sub.2 NHOMe  Gb                                                    CH.sub.2 CH.sub.2 SO.sub.2 NHOMe                                                                        Gb                                                    CH.sub.2 SO.sub.2 NMe.sub.2                                                                             Ga                                                    CH.sub.2 CH.sub.2 SO.sub.2 NMe.sub.2                                                                    Ga                                                    CH.sub.2 SO.sub.2 N(OMe)Me                                                                              Ga                                                    CH.sub.2 CH.sub.2 SO.sub.2 N(OMe)Me                                                                     Ga                                                    CH.sub.2 CONHMe          Gb                                                    CH.sub.2 CH.sub.2 CONHMe Gb                                                    CH.sub.2 CONMe.sub.2     Ga                                                    CH.sub.2 CH.sub.2 CONMe.sub.2                                                                           Ga                                                    CH.sub.2 CONHOMe         Gb                                                    CH.sub.2 CH.sub.2 CONHOMe                                                                               Gb                                                    CH.sub.2 CON(OMe)Me      Ga                                                    CH.sub.2 CH.sub.2 CON(OMe)Me                                                                            Ga                                                    CH.sub.2 NHMe            Gb                                                    CH.sub.2 CH.sub.2 NHMe   Gb                                                    CH.sub.2 NHOMe           Gb                                                    CH.sub.2 CH.sub.2 NHOMe  Gb                                                    CH.sub.2 NMe.sub.2       Ga                                                    CH.sub.2 CH.sub.2 NMe.sub.2                                                                             Ga                                                    CH.sub.2 N(OMe)Me        Ga                                                    CH.sub.2 CH.sub.2 N(OMe)Me                                                                              Ga                                                    CH.sub.2 NMeCOMe         Ga                                                    CH.sub.2 CH.sub.2 NMeCOMe                                                                               Ga                                                    CH.sub.2 N(OMe)COMe      Ga                                                    CH.sub.2 CH.sub.2 N(OMe)COMe                                                                            Ga                                                    CH.sub.2 NMeSO.sub.2 Me  Ga                                                    CH.sub.2 CH.sub.2 NMeSO.sub.2 Me                                                                        Ga                                                    CH.sub.2 N(OMe)SO.sub.2 Me                                                                              Ga                                                    CH.sub.2 CH.sub.2 N(OMe)SO.sub.2 Me                                                                     Ga                                                    CH.sub.2 Ph              Gb                                                    CH.sub.2 CH.sub.2 Ph     Gb                                                    CH.sub.2 CH.sub.2 CH.sub.2 Ph                                                                           Gb                                                    CHMePh                   Gb                                                    CH.sub.2 CHCHPh          Gb                                                    CHMeCHCHPh               Gb                                                    CH.sub.2 CH.sub.2 OPh    Gb                                                    CH.sub.2 OPh             Gb                                                    CH.sub.2 CH.sub.2 SPh    Gb                                                    CH.sub.2 SPh             Gb                                                    CH.sub.2 CH.sub.2 SO.sub.2 Ph                                                                           Gb                                                    CH.sub.2 COPh            Gb                                                    CH.sub.2 CH.sub.2 COPh   Gb                                                    CH.sub.2 COCH.sub.2 Ph   Gb                                                    CH.sub.2 CH.sub.2 COCH.sub.2 Ph                                                                         Gb                                                    ______________________________________                                    

                  TABLE 4C                                                         ______________________________________                                          ##STR947##                                                                     ##STR948##                                                                     ##STR949##                                                                     ##STR950##                                                                     ##STR951##                                                                    R.sup.g1          Gn                                                           ______________________________________                                         Me                Ga                                                           Et                Ga                                                           Pr-n              Ga                                                           Pro-iso           Gb                                                           Bu-n              Ga                                                           Bu-iso            Ga                                                           Pen-n             Gb                                                           CH.sub.2 Pr-cyc   Ga                                                           CH.sub.2 CH.sub.2 Pr-cyc                                                                         Gb                                                           CH.sub.2 CHCH.sub.2                                                                              Ga                                                           CH.sub.2 CHCHMe   Ga                                                           CH.sub.2 CCHMe    Ga                                                           CH.sub.2 C CH     Ga                                                           CH.sub.2 C CMe    Ga                                                           CH.sub.2 CH.sub.2 OMe                                                                            Ga                                                           CH.sub.2 OMe      Ga                                                           CH.sub.2 CH.sub.2 SMe                                                                            Ga                                                           CH.sub.2 SMe      Ga                                                           CH.sub.2 SO.sub.2 Me                                                                             Ga                                                           CH.sub.2 CH.sub.2 SO.sub.2 Me                                                                    Ga                                                           CH.sub.2 CF.sub.3 Ga                                                           CH.sub.2 CN       Ga                                                           CH.sub.2 CH.sub.2 CN                                                                             Ga                                                           CH.sub.2 NO.sub.2 Ga                                                           CH.sub.2 CH.sub.2 NO.sub.2                                                                       Ga                                                           CH.sub.2 COMe     Ga                                                           CH.sub.2 COEt     Ga                                                           CH.sub.2 COCHCH.sub.2                                                                            Ga                                                           CH.sub.2 CHCHCOMe Ga                                                           CH.sub.2 CONMe.sub.2                                                                             Ga                                                           ______________________________________                                    

                  TABLE 5                                                          ______________________________________                                          ##STR952##                                                                     ##STR953##                                                                     ##STR954##                                                                     ##STR955##                                                                     ##STR956##                                                                     ##STR957##                                                                     ##STR958##                                                                     ##STR959##                                                                     ##STR960##                                                                     ##STR961##                                                                     ##STR962##                                                                     ##STR963##                                                                     ##STR964##                                                                     ##STR965##                                                                     ##STR966##                                                                     ##STR967##                                                                     ##STR968##                                                                     ##STR969##                                                                     ##STR970##                                                                     ##STR971##                                                                     ##STR972##                                                                     ##STR973##                                                                     ##STR974##                                                                     ##STR975##                                                                     ##STR976##                                                                     ##STR977##                                                                     ##STR978##                                                                     ##STR979##                                                                     ##STR980##                                                                     ##STR981##                                                                     ##STR982##                                                                     ##STR983##                                                                     ##STR984##                                                                     ##STR985##                                                                     ##STR986##                                                                     ##STR987##                                                                     ##STR988##                                                                     ##STR989##                                                                     ##STR990##                                                                     ##STR991##                                                                     ##STR992##                                                                     ##STR993##                                                                     ##STR994##                                                                     ##STR995##                                                                     ##STR996##                                                                    R.sup.m         L           Gn                                                 ______________________________________                                         Me              Me          Ga                                                 Me              Et          Gb                                                 Et              Me          Ga                                                 Et              Et          Gb                                                 Pr-n            Me          Ga                                                 Pr-n            Et          Gb                                                 Pr-n            CH.sub.2 CHCH.sub.2                                                                        Gb                                                 Pr-n            CH.sub.2 C CH                                                                              Gb                                                 Bu-n            Me          Ga                                                 Bu-n            Et          Gb                                                 Bu-n            CH.sub.2 CHCH.sub.2                                                                        Gb                                                 Bu-n            CH.sub.2 C CH                                                                              Gb                                                 Pen-n           Me          Gb                                                 CH.sub.2 CHCH.sub.2                                                                            Me          Ga                                                 CH.sub.2 CHCH.sub.2                                                                            Et          Gb                                                 CH.sub.2 CHCH.sub.2                                                                            CH.sub.2 CHCH.sub.2                                                                        Gb                                                 CH.sub.2 CHCH.sub.2                                                                            CH.sub.2 C CH                                                                              Gb                                                 CH.sub.2 C CH   Me          Gb                                                 CH.sub.2 C CH   Et          Gb                                                 CH.sub.2 C CH   CH.sub.2 CHCH.sub.2                                                                        Gb                                                 CH.sub.2 C CH   CH.sub.2 C CH                                                                              Gb                                                 CH.sub.2 CH.sub.2 OMe                                                                          Me          Gb                                                 CH.sub.2 CH.sub.2 SMe                                                                          Me          Gb                                                 CH.sub.2 SO.sub.2 Me                                                                           Me          Gb                                                 CH.sub.2 CF.sub.3                                                                              Me          Gb                                                 CH.sub.2 CF.sub.3                                                                              Et          Gb                                                 CH.sub.2 CF.sub.3                                                                              CH.sub.2 CHCH.sub.2                                                                        Gb                                                 CH.sub.2 CF.sub.3                                                                              CH.sub.2 C CH                                                                              Gb                                                 CH.sub.2 CN     Me          Gb                                                 CH.sub.2 COMe   Me          Gb                                                 CH.sub.2 COMe   Et          Gb                                                 CH.sub.2 COMe   CH.sub.2 CHCH.sub.2                                                                        Gb                                                 CH.sub.2 COMe   CH.sub.2 C CH                                                                              Gb                                                 CH.sub.2 COCHCH.sub.2                                                                          Me          Gb                                                 CH.sub.2 CONMe.sub.2                                                                           Me          Gb                                                 ______________________________________                                          R.sup.m represents R.sup.a1, R.sup.b1, R.sup.d1, R.sup.e1 or R.sup.f1.   

                  TABLE 6                                                          ______________________________________                                          ##STR997##                                                                     ##STR998##                                                                     ##STR999##                                                                     ##STR1000##                                                                    ##STR1001##                                                                    ##STR1002##                                                                    ##STR1003##                                                                    ##STR1004##                                                                    ##STR1005##                                                                    ##STR1006##                                                                    ##STR1007##                                                                    ##STR1008##                                                                    ##STR1009##                                                                    ##STR1010##                                                                    ##STR1011##                                                                    ##STR1012##                                                                    ##STR1013##                                                                    ##STR1014##                                                                   R.sup.c1        L           Gn                                                 ______________________________________                                         Me              Me          Ga                                                 Me              Et          Gb                                                 Me              CH.sub.2 CHCH.sub.2                                                                        Gb                                                 Me              CH.sub.2 C CH                                                                              Gb                                                 Et              Me          Ga                                                 Et              Et          Gb                                                 Et              CH.sub.2 CHCH.sub.2                                                                        Gb                                                 Et              CH.sub.2 C CH                                                                              Gb                                                 Pr-n            Me          Ga                                                 Pr-n            Et          Gb                                                 Bu-n            Me          Ga                                                 Bu-n            Et          Gb                                                 Pen-n           Me          Gb                                                 CH.sub.2 CHCH.sub.2                                                                            Me          Ga                                                 CH.sub.2 CHCH.sub.2                                                                            Et          Gb                                                 CH.sub.2 CHCH.sub.2                                                                            CH.sub.2 CHCH.sub.2                                                                        Gb                                                 CH.sub.2 CHCH.sub.2                                                                            CH.sub.2 C CH                                                                              Gb                                                 CH.sub.2 C CH   Me          Gb                                                 CH.sub.2 C CH   Et          Gb                                                 CH.sub.2 C CH   CH.sub.2 CHCH.sub.2                                                                        Gb                                                 CH.sub.2 C CH   CH.sub.2 C CH                                                                              Gb                                                 CH.sub.2 CH.sub.2 OMe                                                                          Me          Gb                                                 CH.sub.2 CH.sub.2 SMe                                                                          Me          Gb                                                 CH.sub.2 SO.sub.2 Me                                                                           Me          Gb                                                 CH.sub.2 CF.sub.3                                                                              Me          Gb                                                 CH.sub.2 CF.sub.3                                                                              Et          Gb                                                 CH.sub.2 CF.sub.3                                                                              CH.sub.2 CHCH.sub.2                                                                        Gb                                                 CH.sub.2 CF.sub.3                                                                              CH.sub.2 C CH                                                                              Gb                                                 CH.sub.2 CN     Me          Gb                                                 CH.sub.2 COMe   Me          Gb                                                 CH.sub.2 COMe   Et          Gb                                                 CH.sub.2 COMe   CH.sub.2 CHCH.sub.2                                                                        Gb                                                 CH.sub.2 COMe   CH.sub.2 C CH                                                                              Gb                                                 CH.sub.2 COCHCH.sub.2                                                                          Me          Gb                                                 CH.sub.2 CONMe.sub.2                                                                           Me          Gb                                                 Ph              Me          Gb                                                 ______________________________________                                    

                  TABLE 7                                                          ______________________________________                                          ##STR1015##                                                                    ##STR1016##                                                                                     ##STR1017##                                                   ##STR1018##                                                                                     ##STR1019##                                                   ##STR1020##                                                                                     ##STR1021##                                                   ##STR1022##                                                                                     ##STR1023##                                                   ##STR1024##                                                                                     ##STR1025##                                                   ##STR1026##                                                                                     ##STR1027##                                                   ##STR1028##                                                                                     ##STR1029##                                                   ##STR1030##                                                                                     ##STR1031##                                                   ##STR1032##                                                                                     ##STR1033##                                                   ##STR1034##                                                                                     ##STR1035##                                                   ##STR1036##                                                                                     ##STR1037##                                                   ##STR1038##                                                                                     ##STR1039##                                                   ##STR1040##                                                                                     ##STR1041##                                                   ##STR1042##                                                                                     ##STR1043##                                                   ##STR1044##                                                                                     ##STR1045##                                                   ##STR1046##                                                                                     ##STR1047##                                                   ##STR1048##                                                                                     ##STR1049##                                                   ##STR1050##                                                                                     ##STR1051##                                                   ##STR1052##                                                                                     ##STR1053##                                                   ##STR1054##                                                                                     ##STR1055##                                                   ##STR1056##                                                                                     ##STR1057##                                                   ##STR1058##                                                                                     ##STR1059##                                                   ##STR1060##                                                                                     ##STR1061##                                                   ##STR1062##                                                                                     ##STR1063##                                                   ##STR1064##                                                                                     ##STR1065##                                                   ##STR1066##                                                                   R.sup.n represents R.sup.d6 or R.sup.f2.                                       R.sup.n         L              Gn                                              ______________________________________                                         Me              Me             Ga                                              Me              Et             Gb                                              Me              CH.sub.2 CHCH.sub.2                                                                           Gb                                              Me              CH.sub.2 CCH   Gb                                              Et              Me             Ga                                              Et              Et             Gb                                              Et              CH.sub.2 CHCH.sub.2                                                                           Gb                                              Et              CH.sub.2 CCH   Gb                                              Pr-n            Me             Ga                                              Pr-n            Et             Gb                                              Pr-n            CH.sub.2 CHCH.sub.2                                                                           Gb                                              Pr-n            CH.sub.2 CCH   Gb                                              CH.sub.2 CHCH.sub.2                                                                            Me             Gb                                              CH.sub.2 CCH    Me             Gb                                              CH.sub.2 SMe    Me             Gb                                              CH.sub.2 CH.sub.2 SMe                                                                          Me             Gb                                              CH.sub.2 SO.sub.2 Me                                                                           Me             Gb                                              CH.sub.2 CH.sub.2 SO.sub.2 Me                                                                  Me             Gb                                              CH.sub.2 OMe    Me             Gb                                              CH.sub.2 CH.sub.2 OMe                                                                          Me             Gb                                              CH.sub.2 CO.sub.2 Me                                                                           Me             Gb                                              CH.sub.2 COMe   Me             Gb                                              CH.sub.2 CH.sub.2 COMe                                                                         Me             Gb                                              CH.sub.2 CN     Me             Gb                                              CH.sub.2 CH.sub.2 CN                                                                           Me             Gb                                              Ph              Me             Gb                                              CH.sub.2 Ph     Me             Gb                                              CH.sub.2 CH.sub.2 Ph                                                                           Me             Gb                                              CHMePh          Me             Gb                                              ______________________________________                                    

                  TABLE 8                                                          ______________________________________                                          ##STR1067##                                                                    ##STR1068##                                                                                     ##STR1069##                                                   ##STR1070##                                                                                     ##STR1071##                                                   ##STR1072##                                                                                     ##STR1073##                                                   ##STR1074##                                                                                     ##STR1075##                                                   ##STR1076##                                                                                     ##STR1077##                                                   ##STR1078##                                                                                     ##STR1079##                                                   ##STR1080##                                                                                     ##STR1081##                                                   ##STR1082##                                                                                     ##STR1083##                                                   ##STR1084##                                                                                     ##STR1085##                                                   ##STR1086##                                                                                     ##STR1087##                                                   ##STR1088##                                                                                     ##STR1089##                                                   ##STR1090##                                                                   R.sup.g1         L             Gn                                              ______________________________________                                         Me               Me            Ga                                              Me               Et            Gb                                              Et               Me            Ga                                              Et               Et            Gb                                              Pr-n             Me            Ga                                              Pr-n             Et            Gb                                              Pr-n             CH.sub.2 CHCH.sub.2                                                                          Gb                                              Pr-n             CH.sub.2 CCH  Gb                                              Bu-n             Me            Ga                                              Bu-n             Et            Gb                                              Bu-n             CH.sub.2 CHCH.sub.2                                                                          Gb                                              Bu-n             CH.sub.2 CCH  Gb                                              Pen-n            Me            Gb                                              CH.sub.2 CHCH.sub.2                                                                             Me            Ga                                              CH.sub.2 CHCH.sub.2                                                                             Et            Gb                                              CH.sub.2 CHCH.sub.2                                                                             CH.sub.2 CHCH.sub.2                                                                          Gb                                              CH.sub.2 CHCH.sub.2                                                                             CH.sub.2 CCH  Gb                                              CH.sub.2 CCH     Me            Gb                                              CH.sub.2 CCH     Et            Gb                                              CH.sub.2 CCH     CH.sub.2 CHCH.sub.2                                                                          Gb                                              CH.sub.2 CCH     CH.sub.2 CCH  Gb                                              CH.sub.2 CH.sub.2 OMe                                                                           Me            Gb                                              CH.sub.2 CH.sub.2 SMe                                                                           Me            Gb                                              CH.sub.2 SO.sub.2 Me                                                                            Me            Gb                                              CH.sub.2 CF.sub.3                                                                               Me            Gb                                              CH.sub.2 CF.sub.3                                                                               Et            Gb                                              CH.sub.2 CF.sub.3                                                                               CH.sub.2 CHCH.sub.2                                                                          Gb                                              CH.sub.2 CF.sub.3                                                                               CH.sub.2 CCH  Gb                                              CH.sub.2 CN      Me            Gb                                              CH.sub.2 COMe    Me            Gb                                              CH.sub.2 COMe    Et            Gb                                              CH.sub.2 COMe    CH.sub.2 CHCH.sub.2                                                                          Gb                                              CH.sub.2 COMe    CH.sub.2 CCH  Gb                                              CH.sub.2 COCHCH.sub.2                                                                           Me            Gb                                              CH.sub.2 CONMe.sub.2                                                                            Me            Gb                                              ______________________________________                                    

                  TABLE 9                                                          ______________________________________                                          ##STR1091##                                                                    ##STR1092##                                                                                     ##STR1093##                                                   ##STR1094##                                                                                     ##STR1095##                                                   ##STR1096##                                                                                     ##STR1097##                                                   ##STR1098##                                                                                     ##STR1099##                                                   ##STR1100##                                                                                     ##STR1101##                                                   ##STR1102##                                                                                     ##STR1103##                                                   ##STR1104##                                                                                     ##STR1105##                                                   ##STR1106##                                                                                     ##STR1107##                                                   ##STR1108##                                                                   R.sup.m represents R.sup.a1, R.sup.b1, R.sup.d1, R.sup.e1 or R.sup.f1.         R.sup.m                 Gn                                                     ______________________________________                                         Me                      Gc                                                     Et                      Gc                                                     Pr-n                    Gc                                                     Pr-iso                  Gc                                                     Bu-n                    Gc                                                     Bu-iso                  Gc                                                     Pen-n                   Gc                                                     CH.sub.2 Pr-cyc         Gc                                                     CH.sub.2 CH.sub.2 Py-cyc                                                                               Gc                                                     CH.sub.2 CHCH.sub.2     Gc                                                     CH.sub.2 CHCHMe         Gc                                                     CH.sub.2 CCH            Gc                                                     CH.sub.2 CCMe           Gc                                                     CH.sub.2 CH.sub.2 OMe   Gc                                                     CH.sub.2 OMe            Gc                                                     CH.sub.2 CH.sub.2 SMe   Gc                                                     CH.sub.2 SMe            Gc                                                     CH.sub.2 SO.sub.2 Me    Gc                                                     CH.sub.2 CH.sub.2 SO.sub.2 Me                                                                          Gc                                                     CH.sub.2 CF.sub.3       Gc                                                     CH.sub.2 CN             Gc                                                     CH.sub.2 CH.sub.2 CN    Gc                                                     CH.sub.2 NO.sub.2       Gc                                                     CH.sub.2 CH.sub.2 NO.sub.2                                                                             Gc                                                     CH.sub.2 COMe           Gc                                                     CH.sub.2 COEt           Gc                                                     CH.sub.2 COCHCH.sub.2   Gc                                                     CH.sub.2 CHCHCOMe       Gc                                                     CH.sub.2 CONMe.sub.2    Gc                                                     ______________________________________                                    

                  TABLE 10                                                         ______________________________________                                          ##STR1109##                                                                    ##STR1110##                                                                                     ##STR1111##                                                   ##STR1112##                                                                                     ##STR1113##                                                   ##STR1114##                                                                   R.sup.c1                Gn                                                     ______________________________________                                         Me                      Gc                                                     Et                      Gc                                                     Pr-n                    Gc                                                     Pr-iso                  Gc                                                     Bu-n                    Gc                                                     Bu-iso                  Gc                                                     Pen-n                   Gc                                                     CH.sub.2 Pr-cyc         Gc                                                     CH.sub.2 CH.sub.2 Py-cyc                                                                               Gc                                                     CH.sub.2 CHCH.sub.2     Gc                                                     CH.sub.2 CHCHMe         Gc                                                     CH.sub.2 CCH            Gc                                                     CH.sub.2 CCMe           Gc                                                     CH.sub.2 CH.sub.2 OMe   Gc                                                     CH.sub.2 OMe            Gc                                                     CH.sub.2 CH.sub.2 SMe   Gc                                                     CH.sub.2 SMe            Gc                                                     CH.sub.2 SO.sub.2 Me    Gc                                                     CH.sub.2 CH.sub.2 SO.sub.2 Me                                                                          Gc                                                     CH.sub.2 CF.sub.3       Gc                                                     CH.sub.2 CN             Gc                                                     CH.sub.2 CH.sub.2 CN    Gc                                                     CH.sub.2 NO.sub.2       Gc                                                     CH.sub.2 CH.sub.2 NO.sub.2                                                                             Gc                                                     CH.sub.2 COMe           Gc                                                     CH.sub.2 COEt           Gc                                                     CH.sub.2 COCHCH.sub.2   Gc                                                     CH.sub.2 CHCHCOMe       Gc                                                     CH.sub.2 CONMe.sub.2    Gc                                                     Ph                      Gc                                                     ______________________________________                                    

                  TABLE 11                                                         ______________________________________                                          ##STR1115##                                                                    ##STR1116##                                                                                      ##STR1117##                                                  ##STR1118##                                                                                      ##STR1119##                                                  ##STR1120##                                                                                      ##STR1121##                                                  ##STR1122##                                                                                      ##STR1123##                                                 R.sup.n represents R.sup.d6 or R.sup.f2.                                              R.sup.n         Gn                                                      ______________________________________                                                Me              Gc                                                             Et              Gc                                                             Pr-n            Gc                                                             CH.sub.2 CHCH.sub.2                                                                            Gc                                                             CH.sub.2 CCH    Gc                                                             CH.sub.2 SMe    Gc                                                             CH.sub.2 CH.sub.2 SMe                                                                          Gc                                                             CH.sub.2 SO.sub.2 Me                                                                           Gc                                                             CH.sub.2 CH.sub.2 SO.sub.2 Me                                                                  Gc                                                             CH.sub.2 OMe    Gc                                                             CH.sub.2 CH.sub.2 OMe                                                                          Gc                                                             CH.sub.2 CO.sub.2 Me                                                                           Gc                                                             CH.sub.2 COMe   Gc                                                             CH.sub.2 CH.sub.2 COMe                                                                         Gc                                                             CH.sub.2 CN     Gc                                                             CH.sub.2 CH.sub.2 CN                                                                           Gc                                                             Ph              Gc                                                             CH.sub.2 Ph     Gc                                                      ______________________________________                                    

                  TABLE 12                                                         ______________________________________                                          ##STR1124##                                                                    ##STR1125##                                                                                     ##STR1126##                                                   ##STR1127##                                                                                     ##STR1128##                                                   ##STR1129##                                                                                     ##STR1130##                                                   ##STR1131##                                                                                     ##STR1132##                                                   ##STR1133##                                                                                     ##STR1134##                                                  R.sup.g1                Gn                                                     ______________________________________                                         Me                      Gc                                                     Et                      Gc                                                     Pr-n                    Gc                                                     Pr-iso                  Gc                                                     Bu-n                    Gc                                                     Bu-iso                  Gc                                                     Pen-n                   Gc                                                     CH.sub.2 Pr-cyc         Gc                                                     CH.sub.2 CH.sub.2 Py-cyc                                                                               Gc                                                     CH.sub.2 CHCH.sub.2     Gc                                                     CH.sub.2 CHCHMe         Gc                                                     CH.sub.2 CCH            Gc                                                     CH.sub.2 CCMe           Gc                                                     CH.sub.2 CH.sub.2 OMe   Gc                                                     CH.sub.2 OMe            Gc                                                     CH.sub.2 CH.sub.2 SMe   Gc                                                     CH.sub.2 SMe            Gc                                                     CH.sub.2 SO.sub.2 Me    Gc                                                     CH.sub.2 CH.sub.2 SO.sub.2 Me                                                                          Gc                                                     CH.sub.2 CF.sub.3       Gc                                                     CH.sub.2 CN             Gc                                                     CH.sub.2 CH.sub.2 CN    Gc                                                     CH.sub.2 NO.sub.2       Gc                                                     CH.sub.2 CH.sub.2 NO.sub.2                                                                             Gc                                                     CH.sub.2 COMe           Gc                                                     CH.sub.2 COEt           Gc                                                     CH.sub.2 COCHCH.sub.2   Gc                                                     CH.sub.2 CHCHCOMe       Gc                                                     CH.sub.2 CONMe.sub.2    Gc                                                     ______________________________________                                    

The compound of the present invention can be used as a herbicide for upland fields by any treating method such as soil treatment, soil admixing treatment or foliage treatment.

The dose of the compound of the present invention varies depending upon the application site, the season for application, the manner of application, the type of weeds to be controlled, the type of crop plants, etc. However, the dose is usually within a range of from 0.0001 to 10 kg, preferably from 0.005 to 5 kg, per hectare (ha), as the amount of the active ingredient.

Further, the compound of the present invention may be combined with other herbicides, various insecticides, fungicides, plant growth regulating agents, synergism agents and safeners at the time of the preparation of the formulations or at the time of the application, as the case requires.

Particularly, by the combined application with other herbicide, it can be expected to reduce the cost due to a decrease of the dose or to enlarge their herbicidal spectrum or obtain higher herbicidal effects due to a synergistic effect of the combined herbicides. In such a case, a plurality of known herbicides may be simultaneously combined. The herbicides of the type which can be used in combination with the compound of the present invention, may, for example, be compounds disclosed in Farm Chemicals Handbook (1990).

When the compound of the present invention is to be used as a herbicide, it is usually mixed with a suitable carrier, for instance, a solid carrier such as clay, talc, bentonite, diatomaceous earth or fine silica powder, or a liquid carrier such as water, an alcohol (such as isopropanol, butanol, benzyl alcohol or furfuryl alcohol), an aromatic hydrocarbon (such as toluene or xylene), an ether (such as anisole), a ketone (such as cyclohexanone or isophorone), an ester (such as butyl acetate), an acid amide (such as N-methylpyrrolidone), or a halogenated hydrocarbon (such as chlorobenzene). If desired, a surfactant, an emulsifier, a dispersing agent, a penetrating agent, a spreader, a thickener, an antifreezing agent, a coagulation preventing agent or a stabilizer may be added to prepare an optional formulation such as a liquid formulation, an emulsifiable concentrate, a wettable powder, a dry flowable, a flowable, a dust or a granule.

Cropland weeds to be controlled by the compound of the present invention include, for example, Solanaceae weeds such as Solanum nigrum and Datura stramonium, Malvaceae weeds such as Abutilon theophrasti and Side spinosa, Convolvulaceae weeds such as Ipomoea spps. e.g. Ipomoea purpurea, and Calystegia spps., Amaranthaceae weeds such as Amaranthus lividus and Amaranthus viridis, Compositae weeds such as Xanthium strumarium, Ambrosia artemisiaefolia, Helianthus annuu, Galinsoga ciliat, Cirsium arvense, Senecio vulgaris and Erigeron annus, Cruciferae weeds such as Rorippa indica, Sinapis arvensis and Capsella Bursapatris, Polygonaceae weeds such as Polygonum Blumei and Polygonum convolvulus, Portulacaceae weeds such as Portulaca oleracea, Chenopodiaceae weeds such as Chenopodium album, Chenopodium ficifolium and Kochia scoparis, Caryophyllaceae weeds such as Stellaria media, Scrophulariaceae weeds such as Veronica persica, Commelinaceae weeds such as Commelina communis, Labiatae weeds such as Lamium amplexicaule and Lamium purpureum, Euphorbiaceae weeds such as Euphorbia supina and Euphorbia maculata, Rubiaceae weeds such as Galium spurium, Galium aparine and Rubia akane, Violaceae weeds such as Viola arvensis, Leguminosae weeds such as Sesbania exaltata and Cassia obtusifolia, Graminaceous weeds such as Sorgham bicolor, Panicum dichotomiflorum, Sorghum halepense, Echinochloa crus-galli, Digitaria adscendens, Avena fatua, Eleusine indica, Setaria viridis and Alopecurus aegualis, and Cyperaceous weeds such as Cyperus rotundus and Cyperus esculentus.

Further, the compound of the present invention can be used as a paddy field herbicide by any treating method such as irrigated soil treatment or foliage treatment. Paddy weeds include, for example, Alismataceae weeds such as Alisma canaliculatum, Sagittaria trifolia and Sagittaria pygmaea, Cyperaceae weeds such as Cyperus difformis, Cyperus serotinus, Scirpus juncoides and Eleocharis kuroguwai, Scrothulariaceae weeds such as Lindemia pyxidaria, Potenderiaceae weeds such as Monochoria vaginalis, Potamogetonaceae weeds such as Potamogeton distinctus, Lythraceae weeds such as Rotala indica, and Gramineae weeds such as Echinochloa crusgalli.

The compound of the present invention can be applied to control various weeds not only in the agricultural and horticultural fields such as upland fields, paddy fields or orchards, but also in non-agricultural fields such as play grounds, non-used vacant fields or railway sides.

The compound of the present invention can easily be produced by selecting any one of the following reaction schemes 1 to 5. ##STR1135## In the above formulas, Q, G and L are as defined above, and Z is a halogen atom.

Namely, the amine (2) is reacted with chlorosulfonyl isocyanate in a solvent such as tetrahydrofuran, dimethoxyethane, acetonitrile, propionitrile, dimethylformamide, dichloromethane, dichloroethane, benzene or toluene and then reacted with the imine (3) or (4) in the presence of a base such as triethylamine, pyridine, sodium hydride, sodium methoxide, sodium ethoxide, sodium hydroxide, potassium hydroxide or potassium carbonate, to obtain the compound of the present invention (l:X=O). ##STR1136## In the above formulas, Q, G, L and Z are as defined above, and Y is a C₁₋₆ alkyl group or a phenyl group.

Namely, the reaction of the imine (3) or (4) with phenyl N-chlorosulfonyl carbamate (5:Y=phenyl group) or an alkyl N-chlorosulfonyl carbamate (5:Y=lower alkyl group), is conducted by using the carbamate derivative (5) in an amount of from 0.5 to 3.0 mols, per mol of the imine (3) or (4). Preferably, the amount is within a range of from 0.9 to 1.2 mols.

The reaction temperature may be selected optionally within a range of from -50° C. to 100° C., but it is preferably within a range of from -20° C. to 30° C.

This reaction can be carried out by using various bases. The amount of the base is from 0.5 to 4.0 mols per mol of the imine (3) or (4).

A suitable base may, for example, be an organic base such as triethylamine or pyridine, a metal hydride such as sodium hydride, an inorganic base such as sodium hydroxide, potassium hydroxide or potassium carbonate, or a metal alkoxide such as sodium methoxide or sodium ethoxide.

A suitable solvent for this reaction is a solvent inert to this reaction, for example, an aromatic hydrocarbon such as benzene, toluene or xylene, a halogenated hydrocarbon such as dichloromethane, chloroform or carbon tetrachloride, an ether such as ethyl ether, isopropyl ether, dioxane or tetrahydrofuran, a nitrile such as acetonitrile or propionitrile, a hydrocarbon such as petroleum ether, petroleum benzine or n-hexane, a ketone such as acetone or methyl ethyl ketone, an ester such as ethyl acetate, or an amide such as dimethylformamide, dimethylacetamide or hexamethyl phosphorous triamide.

These solvents may be used alone or in combination as a mixture.

Particularly preferred is an ether or an amide.

Then, the phenyl N-substituted iminosulfonyl carbamate (6:X=O, Y=phenyl group) or the alkyl N-substituted iminosulfonyl carbamate (6:X=O, Y=lower alkyl group) and the compound (2) are heated in a solvent such as benzene, toluene or dioxane to obtain the compound of the present invention (l:X=O). ##STR1137## In the above formulas, Q, G, L and Y are as defined above.

Namely, the substituted iminosulfonamide derivative (7) is reacted with the carbamate derivative (8) in a solvent such as acetone, acetonitrile or dioxane in the presence of an inorganic base such as potassium carbonate or an organic base such as triethylamine or 1,8-diazabicylo[5.4.0]-7-undecene (DBU) to obtain the compound of the present invention (l:X=O). ##STR1138## In the above formulas, Q, G, L, X and Y are as defined above.

Namely, the substituted iminosulfonamide derivative (7) is reacted with chloroformic acid (thio)ester or carbonic acid (thio)ester in a solvent such as acetone, methyl ethyl ketone, acetonitrile, dioxane or tetrahydrofuran in the presence of a base such as potassium carbonate, triethylamine or pyridine to obtain the compound (6), which is then heated together with the compound (2) in a solvent such as toluene, benzene or dioxane to obtain the compound of the present invention (1). ##STR1139## In the above formulas, Q and G are as defined above.

Namely, the substituted iminosulfonamide derivative (7) is reacted with the isothiocyanate derivative (9) in a solvent such as acetone, acetonitrile, dioxane or tetrahydrofuran in the presence of an inorganic base such as potassium carbonate or an organic base such as triethylamine or DBU, to obtain the compound of the present invention (l:X=S, L=H).

The intermediates to be used in the present invention, i.e. the substituted iminosulfonamide derivative (7), the phenyl N-substituted iminosulfonyl(thio)carbamate (6:Y=phenyl group) and the alkyl N-substituted iminosulfonyl(thio)carbamate (6:Y=C₁₋₆ alkyl group) are also novel compounds.

The substituted iminosulfonamide derivative (7) can be synthesized from an imine (3) or (4) by the methods of the following Reaction Schemes 6 and 7. ##STR1140## In the above formulas, Q and Z are as defined above.

In the Reaction Scheme 6, the reaction of tertbutanol with chlorosulfonyl isocyanate can be conducted by a method per se known, for example, in accordance with Japanese Unexamined Patent Publication No. 101323/1975.

The reaction of the imine (3) or (4) with tertbutylsulfamoyl chloride is carried out by using tertbutylsulfamoyl chloride in an amount of from 0.5 to 3.0 mols per mol of the imine (3) or (4). Preferably the amount is within a range of from 0.9 to 1.2 mols.

The reaction temperature may be selected optionally within a range of from -50° C. to 100° C. However, the temperature is preferably within a range of from -20° C. to 30° C.

This reaction can be conducted by using various bases. The amount of the base is from 0.5 to 4.0 mols per mol of the imine (3) or (4). Preferably, the amount is within a range of from 0.8 to 2.5 mols. A suitable base may, for example, be a metal hydride such as sodium hydride, an organic base such as triethylamine or pyridine, an inorganic base such as sodium hydroxide, potassium hydroxide or potassium carbonate, or a metal alkoxide such as sodium methoxide or sodium ethoxide.

A suitable solvent for the reaction is a solvent inert to this reaction, for example, an aromatic hydrocarbon such as benzene, toluene or xylene a halogenated hydrocarbon such as dichloromethane, chloroform or carbon tetrachloride, an ether such as ethyl ether, isopropyl ether, dioxane or tetrahydrofuran, a nitrile such as acetonitrile or propionitrile, a hydrocarbon such as petroleum ether, petroleum benzine or n-hexane, a ketone such as acetone or methyl ethyl ketone, an ester such as ethyl acetate, or an amide such as dimethylformamide, dimethylacetamide or hexamethylphosphorous triamide.

These solvents may be used alone or in combination as a mixture. Particularly preferred is an ether or an amide. ##STR1141## In the above formulas, Q is as defined above.

In the Reaction Scheme 7, removal of the tert-butyl group is carried out by using trifluoroacetic acid.

The amount of trifluoroacetic acid may be selected optionally within a range of an equimolar amount to an excess amount. Trifluoroacetic acid may be used as a solvent without any particular problem.

The reaction temperature may be selected optionally within a range of from about -50° C. to 80° C. The temperature is preferably within a range of from -20° C. to 30° C.

When a solvent is used for this reaction, a solvent inert to this reaction, for example, an aromatic hydrocarbon such as benzene, toluene or xylene, a halogenated hydrocarbon such as dichloromethane, chloroform or carbon tetrachloride, an ether such as ethyl ether, isopropyl ether, dioxane or tetrahydrofuran, a nitrile such as acetonitrile or propionitrile, a hydrocarbon such as petroleum ether, petroleum benzine or n-hexane, a ketone such as acetone or methyl ethyl ketone, an ester such as ethyl acetate, or an amide such as dimethylformamide, dimethylacetamide or hexamethylphosphorous triamide, may be used. These solvents may be used alone or in combination as a mixture.

In Reaction Scheme 2, the phenyl N-chlorosulfonyl carbamate (5:Y=phenyl group) and the alkyl N-chlorosulfonyl carbamate (5:Y=lower alkyl group) can be synthesized by a method known per se, for example, in accordance with Chemische Berichte, vol. 96, p. 56 (1963).

The imines (3) and (4) to be used as the starting materials for the above reaction, can be synthesized, for example, in accordance with U.S. Pat. No. 4,237,302, Journal of Chemical Society, p. 307 (1956), Chemical and Pharmaceutical Bulletin, vol. 26, p. 3658 (1978), Journal of Organic Chemistry, vol. 30, p. 4298 (1965), East German Patent 291,757, Journal of American Chemical Society, vol. 93, p. 5552 (1971), U.S. Pat. No. 4,054,652, British Patent 752,003, Chemische Berichte, vol. 92, p. 1928 (1959), Journal of Medicinal Chemistry, vol. 6, p. 266 (1963), Chemical Abstracts, vol. 64, 1417le (1966), and Belgain Patent 654,416.

As representative examples, synthetic schemes for 2-imino-3-ethoxythiazolidine hydrobromide, 2-imino-3-n-propoxythiazolidine hydrobromide and 2-imino-3-methoxy-4,5-dimethylthiazoline hydrochloride will be shown as Reaction Schemes 8, 9 and 10. ##STR1142##

THE BEST MODE FOR CARRYING OUT THE INVENTION

Now, syntheses of the compounds of the present invention will be described in detail as Reference Examples and working Examples. However, the present invention is by no means restricted to such specific Examples.

REFERENCE EXAMPLE a-1 ##STR1143##

In 125 ml of dimethylformamide, 50 g (0.5 mol) of 2-aminothiazole was dissolved, and 90 g (0.63 mol) of methyl iodide was added thereto at room temperature. The mixture was further stirred at room temperature for 48 hours. Then, 1000 ml of ethyl acetate was added to the reaction mixture. Formed crystals were collected by filtration, washed with ethyl acetate and then dried to obtain 105 g of 2-imino-3-methylthiazol-4-ine hydroiodide.

Melting point: 181°-183° C.

The 2-imino-3-methylthiazol-4-ine hydroiodide was neutralized with potassium carbonate to obtain 2-imino-3-methylthiazol-4-ine.

Boiling point 55°-60° C./lmmHg

REFERENCE EXAMPLE a-2 ##STR1144##

In 25 ml of dimethylformamide, 8.2 g (80 mmol) of 2-amino-2-thiazolidine was dissolved, and 18.4 g (100 mmol) of n-butyl iodide was added thereto at room temperature. The reaction mixture was heated and stirred at 60° C. for 10 hours and then left to cool to room temperature. The reaction mixture was added to 300 ml of ethyl acetate, and the mixture was stirred at room temperature for 10 minutes. A formed oil substance was separated by decantation from the ethyl acetate solution, and the same operation was repeated twice. Then, ethyl acetate contained in the oil substance was distilled off under reduced pressure to obtain 2-imino-3-n-butylthiazolidine hydroiodide as a crude product.

Then, the 2-imino-3-n-butylthiazolidine hydroiodide was stirred together with 5.28 g (80 mmol) of 85% potassium hydroxide in 300 ml of methanol at room temperature for one hour. Methanol was distilled off under reduced pressure. Then, 200 ml of chloroform was added to the residue, and precipitated insoluble matters were removed by filtration. Chloroform was distilled off under reduced pressure, and 6.9 g of 2-imino-3-n-butylthiazolidine was obtained by distillation under reduced pressure.

Boiling point: 85°-89° C./0.26 torr

REFERENCE EXAMPLE a-3 ##STR1145##

16.9 g (150 mmol) of creatinine was dissolved in 100 ml of N,N-dimethylformamide. Then, 27.6 g (194 mmol) of methyl iodide was added thereto, and the mixture was heated to 50° C. and stirred at that temperature for 2 hours and further at room temperature overnight. To the reaction mixture, 500 ml of ethyl acetate was added, and crystals were collected by filtration. The obtained crystals were washed with ethyl acetate and dried to obtain 26.2 g of 2-imino-1,3-dimethylimidazolidin-4-one hydroiodide as white crystals.

Then, to 150 ml of a methanol solution containing 5.17 g (78.4 mmol) of 85% potassium hydroxide, 20 g (78.4 mmol) of 2-imino-1,3-dimethylimidazolidin-4-one hydroiodied was added, and the mixture was stirred at room temperature for 20 minutes. The solvent was distilled off under reduced pressure. Then, to the residue, 200 ml of chloroform was added, and insoluble matters were filtered off. The filtrate was drived over anhydrous magnesium sulfate, and the solvent was distilled off under reduced pressure to obtain 9.0 g of 2-imino-1,3-dimethylimidazolidin-4-one.

800 mg (21.0 mmol) of lithium aluminum hydride was suspended in 20 ml of dry tetrahydrofuran, and 200 ml of a dry tetrahydrofuran solution containing 1.5 g (11.8 mmol) of 2-imino-1,3-dimethylimidazolidin-4-one, was added thereto at room temperature. The mixture was stirred at the same temperature overnight. Then, to the reaction mixture, 10 ml of ethyl acetate and then 5 ml of water were carefully added, and insoluble matters were filtered off. The filtrate was adjusted to pH 3 with concentrated hydrochloric acid, and then the solvent was distilled off under reduced pressure. Obtained crystals were washed with a solvent mixture of ethyl ether and ethanol to obtain 1.2 g of 2-imino-1,3-dimethylimidazol-4-ine hydrochloride.

Melting point: 168°-171° C.

The structures and the physical property values or characteristics of the compounds prepared by the same methods as the above Reference Examples a-1 to a-3 are presented in Tables 13a-1, 13a-2 and 13a-3.

                  TABLE 13a-1                                                      ______________________________________                                          ##STR1146##                                                                                                    Physical property                                                              values or                                     R.sup.a1     R.sup.a2                                                                              R.sup.a3                                                                               HZ   characteristics                               ______________________________________                                         C.sub.2 H.sub.5                                                                             H      H       HI   m.p. 113-114° C.                       C.sub.3 H.sub.7 -n                                                                          H      H       HI   m.p.  99-101° C.                       CH.sub.2 Ph  H      H       HBr  m.p. 153-155° C.                       CH.sub.2 CO.sub.2 CH.sub.3                                                                  H      H       HBr  m.p. 174-177° C.                       CH.sub.2 CHCH.sub.2                                                                         H      H       HI   m.p. 113-116° C.                       CH.sub.2 CCH H      H       HBr  m.p. 148-153° C.                       CH.sub.2 CO.sub.2 C.sub.2 H.sub.5                                                           H      H       HBr  m.p. 166-167° C.                       CH(CH.sub.3)CO.sub.2 C.sub.2 H.sub.5                                                        H      H       HBr  m.p. 138-141° C.                       CH.sub.2 COCH.sub.3                                                                         H      H       HBr  m.p. 139-141° C.                       CH.sub.3     CH.sub.3                                                                              H       HI   m.p. 157-160° C.                       CH.sub.3     CH.sub.3                                                                              CH.sub.3                                                                               HI   m.p. 208-210° C.                       C.sub.3 H.sub.7 -n                                                                          CH.sub.3                                                                              H       HI   m.p. 166-168° C.                       C.sub.4 H.sub.9 -n                                                                          H      H       HI   m.p.  55-58° C.                        C.sub.5 H.sub.11 -n                                                                         H      H       --   b.p.  97-100° C.                                                             /0.9 torr                                CH.sub.2 CHCHCH.sub.3                                                                       H      H       HBr  m.p. 127-128° C.                       CH.sub.2 CHCHPh                                                                             H      H       HBr  m.p. 125-129° C.                       CH.sub.2 CH.sub.2 OCH.sub.3                                                                 H      H       HBr  m.p. 141-142° C.                       C.sub.3 H.sub.7 -n                                                                          CH.sub.3                                                                              CH.sub.3                                                                               HI   m.p. 135-138° C.                       CH.sub.3     Ph     H       HI   m.p. 235-238° C.                       CH.sub.3     H      Cl      HI   m.p. 225-228° C.                       CH.sub.2 COPh                                                                               H      H       HBr  m.p. 207-208° C.                       CH.sub.2 OCH.sub.2 Ph                                                                       H      H       HCl  m.p.  99-104° C.                       CH.sub.3     H      Br      HI   m.p. 223-225° C.                       C.sub.3 H.sub.7 -n                                                                          H      Cl      HI   m.p. 182-184° C.                       CH(CH.sub.3).sub.2                                                                          H      H       --   b.p.  75-78° C.                                                              /0.3 torr                                CH.sub.2 CN  H      H       HBr  m.p. 154-155° C.                       CH.sub.2 CH(CH.sub.3).sub.2                                                                 H      H       --   b.p.  78-81° C.                                                              /0.3 torr                                C.sub.6 H.sub.13 -n                                                                         H      H       --   b.p. 110-112° C.                                                             /0.45 torr                               CH(CH.sub.3)C.sub.2 H.sub.5                                                                 H      H       --   b.p.  83-90° C.                                                              /0.4 torr                                CH.sub.2 OCH.sub.3                                                                          H      H       --   b.p.  80-81° C.                                                              /0.5 torr                                CH.sub.2 C(Cl)CH.sub.2                                                                      H      H       HCl  m.p. 155-159° C.                       CH.sub.2 CHCHCl                                                                             H      H       HCl  m.p.  60-66° C.                        CH.sub.2 SCH.sub.3                                                                          H      H       --   b.p.  82-85° C.                                                              /0.6 torr                                CH.sub.2 C(CH.sub.3)CH.sub.2                                                                H      H       HCl  m.p. 114-118° C.                       CH.sub.2 CHC(CH.sub.3).sub.2                                                                H      H       --   b.p.  90-102° C.                                                             /0.3 torr                                CH.sub.3     H      CH.sub.3                                                                               HI   m.p. 179-181° C.                       C.sub.3 H.sub.7 -n                                                                          H      CH.sub.3                                                                               HI   m.p. 152-154° C.                       CH.sub.3     H      OCH.sub.3                                                                              HI   m.p. 158-160° C.                       CH.sub.2 PhOMe-p                                                                            H      H       HCl  m.p. 163-165° C.                       CH.sub.2 PhCl-p                                                                             H      H       HCl  m.p. 157-159° C.                       CH.sub.2 C(Br)CH.sub.2                                                                      H      H       HBr  m.p. 165-168° C.                       CH.sub.2 CH.sub.2 Ph                                                                        H      H       HBr  m.p. 144-145° C.                       CH.sub.2 OC.sub.2 H.sub.5                                                                   H      H       HCl  m.p.  95-97° C.                        CH.sub.2 CCCH.sub.3                                                                         H      H       HBr  m.p. 167-169° C.                       ______________________________________                                    

                  TABLE 13a-2                                                      ______________________________________                                          ##STR1147##                                                                                                    Physical property                                                              values or                                     R.sup.a1    R.sup.a4                                                                              R.sup.a5                                                                               HZ    characteristics                               ______________________________________                                         CH.sub.3    H      H       HI    m.p. 147-150° C.                       C.sub.3 H.sub.7 -n                                                                         H      H       HI    m.p. 119-123° C.                       CH.sub.2 CHCH.sub.2                                                                        H      H       HI    m.p. 111-116° C.                       CH.sub.2 CCH                                                                               H      H       HBr   m.p. 118-122° C.                       C.sub.2 H.sub.5                                                                            H      H       --    b.p.  78-83° C.                                                              /0.9 torr                                CH.sub.2 COCH.sub.3                                                                        H      H       HBr   m.p. 233-237° C.                       C.sub.5 H.sub.11 -n                                                                        H      H       --    b.p.  95-96° C.                                                              /0.25 torr                               CH.sub.2 CHCHCH.sub.3                                                                      H      H       --    b.p.  85-90° C.                                                              /0.2 torr                                C.sub.6 H.sub.13 -n                                                                        H      H       --    b.p. 109-110° C.                                                             /0.4 torr                                CH.sub.3    H      CH.sub.3                                                                               --    Pale yellow oil                               C.sub.3 H.sub.7 -n                                                                         H      CH.sub.3                                                                               --    Pale yellow oil                               CH.sub.2 OCH.sub.3                                                                         H      H       HCl   White solid                                   CH.sub.2 C(Cl)CH.sub.2                                                                     H      H       HCl   m.p. 150-155° C.                       CH.sub.2 CHCHCl                                                                            H      H       HCl   m.p. 131-133° C.                       Ph          H      H       HCl   m.p. 224-226° C.                       ______________________________________                                    

                  TABLE 13a-3                                                      ______________________________________                                          ##STR1148##                                                                                                    Physical property values                      R.sup.a1                                                                              R.sup.a2                                                                              R.sup.a3                                                                               R.sup.a6                                                                            HZ    or characteristics                            ______________________________________                                         C.sub.2 H.sub.5                                                                       H      H       CH.sub.3                                                                            HCl   Pale yellow solid                             C.sub.3 H.sub.7 -n                                                                    H      H       CH.sub.3                                                                            HCl   Pale yellow solid                             ______________________________________                                    

REFERENCE EXAMPLE b-1 ##STR1149##

In 40 ml of dimethylformamide, 8.1 g (80 mmol) of 2-aminothiadiazole was dissolved, and 17.0 g (100 mmol) of n-propyl iodide was added thereto at room temperature. The mixture was heated at 60° C. for 30 minutes and then left to cool, and then it was stirred at room temperature for 24 hours. Then, to the reaction mixture, 500 ml of ethyl acetate was added. Formed crystals were collected by filtration, washed with ethyl acetate and then dried to obtain 13.1 g of desired 2-imino-3-n-propylthiadiazol-4-ine hydroiodide. Melting point: 121°-124° C.

The structures and the physical property values of the compounds prepared by the same method as in the above Reference Example b-1 are presented in Table 13.

                  TABLE 13b                                                        ______________________________________                                          ##STR1150##                                                                                              Physical property values                            R.sup.b1   R.sup.b2                                                                               HZ      or characteristics                                  ______________________________________                                         CH.sub.3   H       HI      m.p. 221-227° C.                             CH.sub.2 CHCH.sub.2                                                                       H       HBr     m.p. 131-132° C.                             CH.sub.2 CCH                                                                              H       HBr     m.p. 114-117° C.                             CH.sub.2 COCH.sub.3                                                                       H       HBr     m.p. 198-200° C.                             CH.sub.3   CH.sub.3                                                                               HI      m.p. 117-121° C.                             ______________________________________                                    

REFERENCE EXAMPLE c-1 ##STR1151##

22 g (197 mmol) of n-propoxyamine hydroxhloride was dissolved in 100 ml of water, and 200 ml of ethylene dichloride was added thereto. Then, 27.2 g (197 mmol) of potassium carbonate was added in several times under cooling, and then 21.3 g (196 mmol) of ethyl chloroformate was dropwise added thereto at a temperature of not higher than 10° C. After raising the temperature to room temperature, the mixture was further stirred at the same temperature for 4 hours. The ethylene dichloride layer was separated, and then the aqueous layer was extracted twice with 100 ml of chloroform. The ethylene dichloride layer and the chloroform layer were put together, and washed with a saturated sodium chloride aqueous solution, and then dried over anhydrous sodium sulfate. Then, the solvent was distilled off under reduced pressure. 27 g of ethyl N-n-propoxycarbamate was obtained by distillation under reduced pressure. Boiling point: 88° C./2.5 mmHg

8.73 g (218 mmol) of 60% sodium hydride was suspended in 200 ml of dry tetrahydrofuran, and 50 ml of a dry tetrahydrofuran solution containing 26.7 g (182 mmol) of ethyl N-n-propoxycarbamate, was dropwise added thereto under cooling with ice at a temperature of not higher than 10° C. After raising the temperature to room temperature, the mixture was stirred at the same temperature for 20 minutes and again cooled with ice. Then, 121.4 g (646 mmol) of 1,2-dibromoethane was added all at once. The temperature was gradually raised and then the mixture was refluxed under heating for 2 hours. The mixture was left to cool to room temperature, and the solvent was partially distilled off under reduced pressure. The residue was poured into 100 ml of ice water and extracted three times with 100 ml of chloroform. The chloroform layer was washed with a saturated sodium chloride aqueous solution and then dried over anhydrous sodium sulfate. The solvent was distilled off under reduced pressure, and then 42.0 g of ethyl N-(2-bromoethyl)-N-n-propoxycarbamate was obtained by distillation under reduced pressure. Boiling point: 97° C./0.4 mmHg

A mixture comprising 41.7 g (164 mmol) of ethyl N-(2-bromoethyl)-N-n-propoxycarbamate, 16.2 g (213 mmol) of thiourea and 200 ml of ethanol, was refluxed under heating for 5 hours. The mixture was left to cool, and then the solvent was distilled off under reduced pressure. Then, 300 ml of chloroform was added to the residue, and the mixture was stirred at room temperature for 10 minutes. After removing insoluble matters by filtration, chloroform was distilled off under reduced pressure. To the residue, ethyl ether and a small amount of water were added for crystallization. Then, the crystals were collected by filtration to obtain 50 g of S-[2-(N-ethoxycarbonyl-N-n-propoxy)aminoethyl]isothiuronium hydrobromide. Melting point: 74°-76° C.

5.0 g (15.2 mmol) of S-[2-(N-ethoxycarbonyl-N-n-propoxy)aminoethyl]isothiuronium hydrobromide and 0.27 g (15.0 mmol) of water were added to 30 ml of a 30% hydrogen bromide/acetic acid solution, and the mixture was heated and stirred at 55° C. for 4 hours. The mixture was left to cool, and acetic acid was distilled off under reduced pressure. To the residue, ethyl ether and a small amount of ethanol were added for crystallization. The crystals were collected by filtration to obtain 3.8 g of S-[2-(N-n-propoxy)aminoethyl]isothiuronium hydrobromide. Melting point: 112°-113° C.

3.8 g (14.7 mmol) of S-[2-(N-n-propoxy)aminoethyl]isothiuronium hydrobromide was added to 60 ml of ethanol, and the mixture was refluxed under heating for 3 hours. The mixture was left to cool, and then ethanol was distilled off under reduced pressure. To the residue, ethyl ether and a small amount of ethanol were added for crystallization. The crystals were collected by filtration to obtain 3.2 g of 2-imino-3-n-propoxythiazolidine hydrobromide. Melting point: 117°-119° C.

REFERENCE EXAMPLE c-2 ##STR1152##

5.67 g (70 mmol) of sodium thiocyanate was dissolved in 12 ml of water, and the solution was heated to 80° C. 5.55 g (60 mmol) of chloroacetone was dropwise added thereto over a period of one hour, and the mixture was stirred at the same temperature for 3 hours. The mixture was cooled to room temperature, and then 60 ml of ethyl ether was added thereto. The aqueous layer was separated and removed. The ethyl ether layer was washed twice with 10 ml of water, and then the solvent was distilled off under reduced pressure to obtain 6.0 g of thiocyanoacetone.

2.30 g (20 mmol) of thiocyanoacetone and 1.67 g (20 mmol) of methoxyamine hydrochloride were dissolved in 10 ml of ethanol, and the solution was refluxed under heating for 5 hours. Ethanol was distilled off under reduced pressure. Then, to the obtained residue, 50 ml of ethyl acetate was added. Precipitated crystals were collected by filtration to obtain 3.34 g of 2-imino-3-methoxy-4-methylthiazol-4-ine hydrochloride. Melting point: 145°-155° C. (decomposed)

The structures and the physical property values of the compounds prepared by the same methods as in Reference Examples c-1 and c-2 are presented in Tables 13c-1, 13c-2 and 13c-3.

                  TABLE 13c-1                                                      ______________________________________                                          ##STR1153##                                                                                                    Physical property                                                              values or                                     R.sup.c1    R.sup.c2                                                                              R.sup.c3                                                                               HZ    characteristics                               ______________________________________                                         C.sub.2 H.sub.5                                                                            H      H       HBr   m.p. 175-176° C.                       CH(CH.sub.3).sub.2                                                                         H      H       HBr   m.p. 150-152° C.                       CH.sub.3    H      H       HBr   Pale yellow glassy                            C.sub.4 H.sub.9 -n                                                                         H      H       HBr   m.p.  97-98° C.                        CH.sub.2 CCH                                                                               H      H       HBr   m.p. 139-140° C.                       CH.sub.2 CHCH.sub.2                                                                        H      H       HBr   m.p. 139-140° C.                       CH.sub.2 CHCHCl                                                                            H      H       HBr   m.p. 145-150° C.                       CH.sub.2 CH(CH.sub.3).sub.2                                                                H      H       HBr   m.p. 110-111° C.                       C.sub.5 H.sub.11 -n                                                                        H      H       HBr   Oil                                           CH.sub.2 C(Cl)CH.sub.2                                                                     H      H       HBr   m.p. 169-170° C.                       CH.sub.2 Ph H      H       HBr   m.p. 167-169° C.                       ______________________________________                                    

                  TABLE 13c-2                                                      ______________________________________                                          ##STR1154##                                                                                                    Physical property values                      R.sup.c1                                                                             R.sup.c4                                                                              R.sup.c5                                                                               R.sup.c6                                                                             HZ    or characteristics                            ______________________________________                                         C.sub.2 H.sub.5                                                                      H      H       H     HBr   m.p. 209-210° C.                       ______________________________________                                    

                  TABLE 13c-3                                                      ______________________________________                                          ##STR1155##                                                                                                 Physical property values                         R.sup.C1                                                                               R.sup.c7                                                                               R.sup.c8                                                                               HZ    or characteristics                               ______________________________________                                         CH.sub.3                                                                               CH.sub.3                                                                               CH.sub.3                                                                               HCl   m.p. 150-155° C.                                                             (decomposed)                                ______________________________________                                    

REFERENCE EXAMPLE d-1 ##STR1156##

11.6 g (0.1 mol) of pseudothiohydantoin was suspended in 150 ml of dimethylformamide, and 17 g (0.12 mol) of methyl iodide was added thereto. Then, the mixture was stirred at 60° C. for one hour. After being left to cool, the reaction mixture was poured into 1000 ml of ethyl acetate, and precipitated crystals were collected by filtration to obtain 15 g of 3-methyl-2-iminothiazolidin-4-one hydroiodide as pale yellow crystals. Melting point: 237°-238° C.

REFERENCE EXAMPLE d-2 ##STR1157##

9.04 g (80 mmol) of creatinine was suspended in 50 ml of dimethylformamide, and 17.0 g (100 mmol) of n-propyl iodide was added thereto. Then, the mixture was heated and stirred within a range of from 70° C. to 80° C. until creatinine was completely dissolved. The mixture was left to cool, and 500 ml of ethyl acetate was added thereto. Precipitated crystals were collected by filtration to obtain 10.6 g of 1-methyl-3-n-propyl-2-iminoimidazolidin-4-one hydroiodide. Melting point: 159°-161° C.

The 1-methyl-3-n-propyl-2-iminoimidazolidin-4-one hydroiodide was neutralized in accordance with the following method to obtain 1-methyl-3-n-propyl-2-iminoimidazolidin-4-one.

2.83 g (10 mmol) of the 1-methyl-3-n-propyl-2-iminoimidazolidin-4-one hydroiodide was added to 25 ml of methanol containing 0.66 g (10 mmol) of 85% potassium hydroxide, and the mixture was stirred at room temperature for one hour. Methanol was distilled off under reduced pressure, and chloroform was added to the residue. Precipitated crystals were removed by filtration. Chloroform was distilled off under reduced pressure to obtain 1.16 g of 1-methyl-3-n-propyl-2-iminoimidazolidin-4-one as an oily substance.

The structures and the physical property values of the compounds prepared by the same methods as in Reference Examples d-1 and d-2, are presented in Table 13d.

                  TABLE 13d                                                        ______________________________________                                          ##STR1158##                                                                                                  Physical property values                        R.sup.d1   R.sup.d4                                                                              R.sup.d5                                                                              HZ    or characteristics                              ______________________________________                                         CH.sub.3   H      CH.sub.3                                                                              HI    m.p. 215-216° C.                         C.sub.2 H.sub.5                                                                           H      CH.sub.3                                                                              HI    m.p. 220-222° C.                         CH.sub.2 CHCH.sub.2                                                                       H      CH.sub.3                                                                              HBr   m.p. 117-119° C.                         CH.sub.2 CCH                                                                              H      CH.sub.3                                                                              HBr   m.p. 228-230° C.                         CH.sub.2 COCH.sub.3                                                                       H      CH.sub.3                                                                              HBr   m.p. 188-190° C.                         CH.sub.2 CO.sub.2 CH.sub.3                                                                H      CH.sub.3                                                                              HBr   m.p. 201-203° C.                         CH.sub.2 OCH.sub.3                                                                        H      CH.sub.3                                                                              HCl   m.p. 198-199° C.                         CH.sub.2 SCH.sub.3                                                                        H      CH.sub.3                                                                              HCl   m.p. 200-210° C.                                                             (decomposed)                               ______________________________________                                          ##STR1159##

1.3 g (11.4 mmol) of 2-amino-6H-1,3-thiazine was dissolved in 4 ml of dimethylformamide, and 2.4 g (14.1 mmol) of n-propyl iodide was added thereto. The mixture was heated at 50° C. for one hour and then stirred at room temperature overnight. To the reaction solution, 100 ml of ethyl acetate was added, and the mixture was stirred and then left to stand still. Then, the ethyl acetate layer was separated and removed by decantation. Then, the residual oily substance was dissolved in 50 ml of methanol, and 30 ml of a methanol solution containing 0.75 g (11.4 mmol) of 85% potassium hydroxide, was added thereto at room temperature. The mixture was further stirred at the same temperature for one hour, and then methanol was distilled off under reduced pressure. To the residue, 60 ml of chloroform was added, and insoluble matters were removed by filtration. Then, the filtrate was concentrated under reduced pressure. The residual oily substance was purified by alumina column chromatography (eluent: chloroform) to obtain 0.4 g of 3,6-dihydro-3-n-propyl-2H-1,3-thiazin-2-imine as an oily substance.

REFERENCE EXAMPLE 2-e ##STR1160##

3.13 g (27 mmol) of 2-amino-4,5-dihydro-6H-1,3-thiazine was dissolved in 20 ml of isopropyl alcohol, and 4.26 g (30 mmol) of methyl iodide was added thereto. The mixture was refluxed under heating for one hour, and then left to cool. The solvent was distilled off under reduced pressure. Then, the residual oily substance was dissolved in 200 ml of methanol, and a 70 ml of a methanol solution containing 1.68 g (25.5 mmol) of 85% potassium hydroxide, was added thereto at room temperature. The mixture was stirred at the same temperature for 5 minutes, and then methanol was distilled off under reduced pressure. To the residue, 300 ml of chloroform was added and then dried over anhydrous sodium sulfate. Inorganic substances were removed by filtration, and then chloroform was distilled off under reduced pressure to obtain 3 g of 3,4,5,6-tetrahydro-3-methyl-2H-1,3-thiazin-2-imine as a pale red oily substance.

The structures and the characteristics of the compounds prepared by the same methods as in Reference Examples e-1 and e-2, are presented in Tables 13e-1 and 13e-2.

                  TABLE 13e-1                                                      ______________________________________                                          ##STR1161##                                                                                                  Physical property values                        R.sup.e1 R.sup.e2                                                                               R.sup.e3                                                                               R.sup.e4                                                                             or characteristics                              ______________________________________                                         CH.sub.3 H       H       H     Oil                                             CH.sub.2 OCH.sub.3                                                                      H       H       H     Oil                                             ______________________________________                                    

                  TABLE 13e-2                                                      ______________________________________                                          ##STR1162##                                                                                                Physical property values                          R.sup.e1                                                                              R.sup.e8                                                                               R.sup.e9                                                                               R.sup.e10                                                                            or characteristics                                ______________________________________                                         C.sub.3 H.sub.7 -n                                                                    H       H       H     Oil                                               ______________________________________                                    

REFERENCE EXAMPLE f-1 ##STR1163##

15 g (122 mmol) of 2-amino-2-oxazoline hydrochloride was stirred with 8.4 g (128 mmol) of 85% potassium hydroxide in 400 ml of methanol at room temperature for one hour. Methanol was distilled off under reduced pressure, and then 500 ml of chloroform was added. Precipitated insoluble substances were removed by filtration. Chloroform was distilled off under reduced pressure to obtain 10.5 g of 2-amino-2-oxazoline.

Then, 10.5 g of 2-amino-2-oxazoline was dissolved in 40 ml of dimethylformamide, and 22 g (155 mmol) of methyl iodide was added thereto at room temperature. The mixture was further stirred at room temperature for 48 hours. Then, 1000 ml of ethyl acetate was added to the reaction mixture. Formed crystals were collected by filtration, washed with ethyl acetate and then dried to obtain 23 g of 2-imino-3-methyloxazolidine hydroiodide. Melting point: 165°-169° C.

The structures and characteristics of the compounds prepared by the same method as in Reference Example f-1 are presented in Table 13f.

                  TABLE 13f                                                        ______________________________________                                          ##STR1164##                                                                                                  Physical property values                        R.sup.f1  R.sup.f5                                                                               R.sup.f6                                                                              HZ    or characteristics                              ______________________________________                                         CH.sub.2 CHCH.sub.2                                                                      H       H      HBr   Glassy                                          ______________________________________                                    

REFERENCE EXAMPLE g-1 ##STR1165##

35 g (0.5 mol) of N,N-dimethylcyanamide was dissolved in a mixed solution of 70 ml of pyridine and 70 ml of triethylamine, and the solution was heated to 60° C. Hydrogen sulfide gas was introduced thereinto for 30 minutes. Then, the reaction mixture was left to cool to room temperature, and 300 ml of ethyl ether was added thereto. Precipitated crystals were collected by filtration and then washed with ethyl ether to obtain 48 g of N,N-dimethylthiourea as pale brown crystals. Melting point: 163°-164° C.

10.4 g (0.1 mol) of N,N-dimethylthiourea was suspended in 80 ml of ethanol, and 17 g (0.12 mol) of methyl iodide was added thereto. The mixture was refluxed under heating for 30 minutes. The reaction mixture was left to cool to room temperature, and then the solvent was distilled off under reduced pressure. The obtained crystals were washed with ethyl ether, collected by filtration and dried to obtain 20 g of N,N-dimethyl-S-methylisothiourea hydroiodide as yellow crystals. Melting point: 84°-85° C.

REFERENCE EXAMPLE q-2 ##STR1166##

7.08 g (120 mmol) of N-ethyl-N-methylamine was dissolved in 80 ml of dry acetone, and the solution was cooled to 0° C. 13.1 g (100 mmol) of ethoxycarbonyl isothiocyanate was dropwise added thereto. Then, the reaction temperature was raised to room temperature, and the mixture was further stirred at the same temperature for 2 hours. The solvent was distilled off under reduced pressure. To the obtained residue, 80 ml of concentrated hydrochloric acid was added. The reaction temperature was raised to 80° C., and the mixture was further stirred at the same temperature for 5 hours. Then, it was cooled to 0° C., and then ammonium carbonate was gradually added to neutralize the reaction mixture (pH=6 to 7). After adding a small amount of water, the mixture was extracted three times with 100 ml of ethyl acetate. The ethyl acetate layer was washed with water and then dried over anhydrous sodium sulfate. Then, the solvent was distilled off under reduced pressure. Obtained crystals were washed with a solvent mixture of ethanol/n-hexane to obtain 5.8 g of N-ethyl-N-methylthiourea as white crystals. Melting point: 124°-125° C.

5.8 g (49 mmol) of N-ethyl-N-methylthiourea was dissolved in 10 ml of N,N-dimethylformamide. 8.8 g (62 mmol) of methyl iodide was added at room temperature, and the mixture was stirred at room temperature for 15 hours. 500 ml of ethyl acetate was added to the mixture, and precipitated crystals were collected by filtration and then washed with ethyl acetate to obtain 3.1 g of N-ethyl-N-methyl-S-methylisothiourea hydroiodide as pale yellow crystals. Melting point: 94°-97° C.

REFERENCE EXAMPLE q-3 ##STR1167##

1.83 g (30 mmol) of N-methoxy-N-methylamine was dissolved in 20 ml of dichloromethane, and the solution was cooled to 0° C. 3.93 g (30 mmol) of ethoxycarbonyl isothiocyanate was dropwise added thereto. Then, the reaction temperature was raised to room temperature, and the mixture was further stirred at the same temperature for 15 hours. The solvent was distilled off under reduced pressure, and to the obtained residue, 20 ml of concentrated hydrochloric acid was added. The reaction temperature was raised to 80° C., and the mixture was further stirred at the same temperature for 5 hours. Then, the mixture was cooled to 0° C., and then ammonium carbonate was gradually added to neutralize the reaction mixture (pH=6 to 7). After adding 10 ml of water, the mixture was extracted three times with 50 ml of ethyl acetate. The ethyl acetate layer was washed with water and then dried over anhydrous magnesium sulfate. Then, the solvent was distilled off under reduced pressure to obtain 2.0 g of N-methoxy-N-methylthiourea as pale yellow crystals. Melting point: 30°-32° C.

1.76 g (14.7 mmol) of N-methoxy-N-methylthiourea was dissolved in 5 ml of N,N-dimethylformamide. 2.09 g (14.7 mmol) of methyl iodide was added thereto at room temperature, and the mixture was stirred at room temperature for 15 hours. 500 ml of ethyl acetate was added thereto, and precipitated crystals were collected by filtration and then washed with ethyl acetate to obtain 2.7 g of N-methoxy-N-methyl-S-methylisothiourea hydroiodide as pale yellow crystals. Melting point: 122°-124° C.

The structures and physical property values or characteristics of the compounds prepared by the same methods as in Reference Examples g-1 to g-3 are presented in Table 13g.

                                      TABLE 13g                                    __________________________________________________________________________      ##STR1168##                                                                                              Physical property values                            R.sup.g1 R.sup.g2 R.sup.g3                                                                            HZ  or characteristics                                  __________________________________________________________________________     C.sub.2 H.sub.5                                                                         CH.sub.3 CH.sub.3                                                                            HI  m.p.                                                                               93-94° C.                                C.sub.3 H.sub.7 -n                                                                      CH.sub.3 CH.sub.3                                                                            HI  m.p.                                                                               54-55° C.                                CH.sub.2 CHCH.sub.2                                                                     CH.sub.3 CH.sub.3                                                                            HBr m.p.                                                                              148-149° C.                               CH.sub.2 CCH                                                                            CH.sub.3 CH.sub.3                                                                            HBr m.p.                                                                              113-114° C.                               CH.sub.3 CH.sub.3 CO                                                                             CH.sub.3                                                                            --  Glassy                                              CH.sub.3 (CH.sub.2).sub.4                                                                             HI  m.p.                                                                              121-123° C.                               CH.sub.3 C.sub.3 H.sub.7 -n                                                                      CH.sub.3                                                                            HI  m.p.                                                                              126-127° C.                               CH.sub.3 Ph       CH.sub.3                                                                            HI  m.p.                                                                              170-173° C.                               CH.sub.3 C.sub.2 H.sub.5 O                                                                       CH.sub.3                                                                            HI  m.p.                                                                              114-115° C.                               CH.sub.3 n-C.sub.3 H.sub.7 O                                                                     CH.sub.3                                                                            HI  m.p.                                                                               75-76° C.                                CH.sub.3 CH.sub.2CHCH.sub.2                                                                      CH.sub.3                                                                            HI  m.p.                                                                              116-118° C.                               __________________________________________________________________________

EXAMPLE a-1 ##STR1169##

1.55 g (10 mmol) of 2-amino-4,6-dimethoxypyrimidine was dissolved in 20 ml of dry tetrahydrofuran, and 1.42 g (10 mmol) of chlorosulfonyl isocyanate was dropwise added thereto within a range of from -10° C. to -5° C. The reaction temperature was raised to 0° C., and the mixture was stirred for 5 minutes. The reaction mixture was again cooled to -30° C., and 1.14 g (10 mmol) of 2-imino-3-methylthiazol-4-ine and 1.11 g (11 mmol) of triethylamine dissolved in 10 ml of dry tetrahydrofuran were dropwise added thereto. The reaction temperature was raised to room temperature, and the mixture was further stirred at the same temperature for one hour. Then, the solvent was distilled off under reduced pressure. Then, water was added to the obtained residue. Precipitated crystals were collected by filtration and washed with acetonitrile to obtain 1.5 g of desired 1-(3-methyl-4-thiazoline-2-sulfonylimino)-3-(4,6-dimethoxyprimidin-2-yl)urea. Melting point: 214°-215° C.

EXAMPLE a-2 ##STR1170##

1.55 g (10 mmol) of 2-amino-4,6-dimethoxypyrimidine was dissolved in 30 ml of dry tetrahydrofuran, and 1.42 g (10 mmol) of chlorosulfonyl isocyanate was dropwise added thereto at a temperature of not higher than -20° C. The reaction temperature was raised to 0° C., and then the mixture was cooled again to a temperature of not higher than -20° C. Then, 2.70 g (10 mmol) of 2-imino-3-n-propylthiazol-4-ine hydroiodide and 2.22 g (22 mmol) of triethylamine dissolved in 30 ml of dry tetrahydrofuran were dropwise added thereto. The reaction temperature was raised to room temperature, and the mixture was further stirred at the same temperature for one hour. Then, the solvent was distilled off under reduced pressure. Then, water was added to the residue, and the mixture was extracted three times with chloroform. The chloroform layer was washed sequentially with water and a saturated sodium chloride aqueous solution and then dried over anhydrous sodium sulfate. Then, the solvent was distilled off under reduced pressure. The obtained crystals were washed with ethyl ether to obtain 3 g of desired 1-(3-n-propyl-4-thiazoline-2-sulfonylimino)-3-(4,6-dimethoxyprimidin-2-yl)urea. Melting point: 166°-167° C.

EXAMPLE a-3 ##STR1171##

1.55 g (10 mmol) of 2-amino-4,6-dimethoxypyrimidine was dissolved in 40 ml of dry tetrahydrofuran, and 1.42 g (10 mmol) of chlorosulfonyl isocyanate was dropwise added thereto at -40° C. The reaction temperature was raised to 0° C., and then the reaction mixture was cooled again to--60° C. Then, 1.90 g (12 mmol) of 2-imino-3-n-butylthiazolidine suspended in 40 ml of dry tetrahydrofuran containing 1.33 g (13 mmol) of triethylamine, was added thereto. The reaction temperature was raised to room temperature, and the mixture was further stirred at the same temperature for one hour. Then, the solvent was distilled off under reduced pressure. Then, water was added to the residue, and the mixture was extracted three times with chloroform. The chloroform layer was washed sequentially with water and a saturated sodium chloride aqueous solution, and then dried over anhydrous sodium sulfate. Then, the solvent was distilled off under reduced pressure. The obtained crystals were washed with ethyl ether to obtain 2.8 g of desired 1-(3-n-butylthiazolidine-2-sulfonylimino)-3-(4,6-dimethoxypyrimidin-2-yl)urea. Melting point: 139°-140° C.

EXAMPLE a-4 ##STR1172##

540 mg (3.46 mmol) of 2-amino-4,6-dimethoxypyrimidine was dissolved in 30 ml of dry tetrahydrofuran, and 490 mg (3.46 mmol) of chlorosulfonyl isocyanate was dropwise added in a range of from -20° C. to -15° C. The reaction temperature was raised to 0° C., and then the mixture was cooled again to -20° C. Then, a mixture comprising 600 mg (4.07 mmol) of 2-imino-1,3-dimethylimidazol-4-ine hydrochloride, 820 mg (8.13 mmol) of triethylamine and 30 ml of dry tetrahydrofuran, was added thereto. The reaction temperature was raised to room temperature, and the mixture was further stirred at the same temperature for 3 hours. Then, the solvent was distilled off under reduced pressure. Then, 60 ml of water was added to the obtained residue, and crystals were collected by filtration. The obtained crystals were washed with a solvent mixture of ethyl ether, acetonitrile and acetone to obtain 200 mg of desired 1-(1,3-dimethyl-4-imidazoline-2-sulfonylimino)-3-(4,6-dimethoxypyrimidin-2-yl)urea. Melting point: 201°-203° C.

The structures and the physical property values of the compounds prepared by the same methods as in Examples a-1 to a-4 are presented in Tables 14a-1, 14a-2 and 14a-3.

                                      TABLE 14a-1                                  __________________________________________________________________________      ##STR1173##                                                                                                                    m.p.                          Compound No.                                                                            R.sup.a1   R.sup.a2                                                                           R.sup.a3                                                                            L   A   B     D     (°C.)                  __________________________________________________________________________      4-a     CH.sub.2 CO.sub.2 CH.sub.3                                                                H   H    H   CH  OCH.sub.3                                                                            OCH.sub.3                                                                            166-167                        5-a     CH.sub.2 Ph                                                                               H   H    H   CH  OCH.sub.3                                                                            OCH.sub.3                                                                            177-178                        6-a     C.sub.2 H.sub.5                                                                           H   H    H   CH  OCH.sub.3                                                                            OCH.sub.3                                                                            189-190                        7-a     CH.sub.2 CHCH.sub.2                                                                       H   H    H   CH  OCH.sub.3                                                                            OCH.sub.3                                                                            165-166                        8-a     CH.sub.2 CCH                                                                              H   H    H   CH  OCH.sub.3                                                                            OCH.sub.3                                                                            183-184                        9-a     CH.sub.2 CO.sub.2 C.sub.2 H.sub.5                                                         H   H    H   CH  OCH.sub.3                                                                            OCH.sub.3                                                                            137-138                       10-a     CH.sub.2 COCH.sub.3                                                                       H   H    H   CH  OCH.sub.3                                                                            OCH.sub.3                                                                            180-181                       11-a     CH(CH.sub.3)CO.sub.2 C.sub.2 H.sub.5                                                      H   H    H   CH  OCH.sub.3                                                                            OCH.sub.3                                                                            131-132                       12-a     C.sub.3 H.sub.7 -n                                                                        H   H    H   CH  OCH.sub.3                                                                            CH.sub.3                                                                             167-170                       13-a     C.sub.3 H.sub.7 -n                                                                        H   H    H   CH  CH.sub.3                                                                             CH.sub.3                                                                             155-158                       14-a     C.sub.3 H.sub.7 -n                                                                        H   H    H   CH  OCHF.sub.2                                                                           OCHF.sub.2                                                                           152-154                       15-a     C.sub.3 H.sub.7 -n                                                                        H   H    H   CH  OCHF.sub.2                                                                           CH.sub.3                                                                             143-145                       16-a     C.sub.3 H.sub.7 -n                                                                        H   H    H   N   OCH.sub.3                                                                            CH.sub.3                                                                             174-176                       17-a     CH.sub.3   CH.sub.3                                                                           H    H   CH  OCH.sub.3                                                                            OCH.sub.3                                                                            211-213                       18-a     CH.sub.3   CH.sub.3                                                                           CH.sub.3                                                                            H   CH  OCH.sub.3                                                                            OCH.sub.3                                                                            203-205                       19-a     C.sub.3 H.sub.7 -n                                                                        CH.sub.3                                                                           H    H   CH  OCH.sub.3                                                                            OCH.sub.3                                                                            176-178                       20-a     C.sub.4 H.sub.9 -n                                                                        H   H    H   CH  OCH.sub.3                                                                            OCH.sub.3                                                                            149-151                       21-a     C.sub.5 H.sub.11 -n                                                                       H   H    H   CH  OCH.sub.3                                                                            OCH.sub.3                                                                            160-161                       22-a     CH.sub.2 CHCHCH.sub.3                                                                     H   H    H   CH  OCH.sub.3                                                                            OCH.sub.3                                                                            123-125                       23-a     CH.sub.2 CHCHPh                                                                           H   H    H   CH  OCH.sub.3                                                                            OCH.sub.3                                                                            180-181                       27-a     CH.sub.2 CH.sub.2 OCH.sub.3                                                               H   H    H   CH  OCH.sub.3                                                                            OCH.sub.3                                                                            137.5-138.5                   28-a     C.sub.3 H.sub.7 -n                                                                        CH.sub.3                                                                           CH.sub.3                                                                            H   CH  OCH.sub.3                                                                            OCH.sub.3                                                                            199-201                       29-a     CH.sub.3   Ph  H    H   CH  OCH.sub.3                                                                            OCH.sub.3                                                                            196-198                       30-a     CH.sub.3   H   Cl   H   CH  OCH.sub.3                                                                            OCH.sub.3                                                                            198-201                       31-a     CH.sub.3   H   Br   H   CH  OCH.sub.3                                                                            OCH.sub.3                                                                            209-211                       32-a     C.sub.3 H.sub.7 -n                                                                        H   Cl   H   CH  OCH.sub.3                                                                            OCH.sub.3                                                                            139-142                       33-a     CH.sub.2 OCH.sub.2 Ph                                                                     H   H    H   CH  OCH.sub.3                                                                            OCH.sub.3                                                                            168-169                       35-a     C.sub.6 H.sub.13 -n                                                                       H   H    H   CH  OCH.sub.3                                                                            OCH.sub.3                                                                            173-175                       36-a     CH.sub.2 CH(CH.sub.3).sub.2                                                               H   H    H   CH  OCH.sub.3                                                                            OCH.sub.3                                                                            177-179                       37-a     CH(CH.sub.3).sub.2                                                                        H   H    H   CH  OCH.sub.3                                                                            OCH.sub.3                                                                            175.5-176.5                   38-a     CH.sub.2 OCH.sub.3                                                                        H   H    H   CH  OCH.sub.3                                                                            OCH.sub.3                                                                            173-174                       39-a     CH(CH.sub.3)C.sub.2 H.sub.5                                                               H   H    H   CH  OCH.sub.3                                                                            OCH.sub.3                                                                            81-82                         43-a     CH.sub.2 SCH.sub.3                                                                        H   H    H   CH  OCH.sub.3                                                                            OCH.sub.3                                                                            181-183                       44-a     CH.sub.2 CN                                                                               H   H    H   CH  OCH.sub.3                                                                            OCH.sub.3                                                                              183-183.5                   45-a     CH.sub.2 C(Cl)CH.sub.2                                                                    H   H    H   CH  OCH.sub.3                                                                            OCH.sub.3                                                                            174-175                       46-a     C.sub.3 H.sub.7 -n                                                                        H   H    CH.sub.3                                                                           CH  OCH.sub.3                                                                            OCH.sub.3                                                                            172-173                       47-a     C.sub.4 H.sub.9 -n                                                                        H   H    H   CH  OCH.sub.3                                                                            CH.sub.3                                                                             147-149                       48-a     CH.sub.2 CHCHCl                                                                           H   H    H   CH  OCH.sub.3                                                                            OCH.sub.3                                                                            165-167                       49-a     CH.sub.2 C(CH.sub.3)CH.sub.2                                                              H   H    H   CH  OCH.sub.3                                                                            OCH.sub.3                                                                            177-179                       52-a     CH.sub.3   H   CH.sub.3                                                                            H   CH  OCH.sub.3                                                                            OCH.sub.3                                                                            206-208                       53-a     C.sub.3 H.sub.7 -n                                                                        H   CH.sub.3                                                                            H   CH  OCH.sub.3                                                                            OCH.sub.3                                                                            152-154                       54-a     CH.sub.3   H   OCH.sub.3                                                                           H   CH  OCH.sub.3                                                                            OCH.sub.3                                                                            187-190                       55-a     CH.sub.2 CHC(CH.sub.3).sub.2                                                              H   H    H   CH  OCH.sub.3                                                                            OCH.sub.3                                                                            170-171                       57-a     CH.sub.2 CH.sub.2 Ph                                                                      H   H    H   CH  OCH.sub.3                                                                            OCH.sub.3                                                                            182-184                       58-a     CH.sub.2 PhOMe-p                                                                          H   H    H   CH  OCH.sub.3                                                                            OCH.sub.3                                                                            109-110                       60-a     CH.sub.2 PhCl-p                                                                           H   H    H   CH  OCH.sub.3                                                                            OCH.sub.3                                                                            182-183                       61-a     CH.sub.2 C(Br)CH.sub.2                                                                    H   H    H   CH  OCH.sub.3                                                                            OCH.sub.3                                                                            167-168                       63-a     CH.sub.2 OC.sub.2 H.sub.5                                                                 H   H    H   CH  OCH.sub.3                                                                            OCH.sub.3                                                                            177-178                       65-a     CH.sub.2 CCCH.sub.3                                                                       H   H    H   CH  OCH.sub.3                                                                            OCH.sub.3                                                                            184-186                       68-a     C.sub.3 H.sub.7 -n                                                                        H   H    H   CH  OCH.sub.3                                                                            Cl    165-168                       72-a     C.sub.3 H.sub.7 -n                                                                        H   H    H   CH  OCH.sub.3                                                                            OCHF.sub.2                                                                           193-195                       73-a     C.sub.3 H.sub.7 -n                                                                        H   H    H   N   OCH.sub.3                                                                            OCH.sub.3                                                                            156-158                       79-a     C.sub.3 H.sub.7 -n                                                                        H   H    H   N   OC.sub.2 H.sub.5                                                                     CH.sub.3                                                                             151-153                       80-a     C.sub.3 H.sub.7 -n                                                                        H   H    H   N   OCH.sub.3                                                                            C.sub.2 H.sub.5                                                                      141-143                       82-a     C.sub.3 H.sub.7 -n                                                                        H   H    H   N   OCH.sub.3                                                                            CH.sub.2 Cl                                                                          144-146                       83-a     C.sub.3 H.sub.7 -n                                                                        H   H    H   CH  CF.sub.3                                                                             Cl    146-148                       84-a     C.sub.3 H.sub.7 -n                                                                        H   H    H   N   OCH.sub.3                                                                            C.sub.3 H.sub.7 -n                                                                   159-160                       85-a     C.sub.3 H.sub.7 -n                                                                        H   H    H   N   OCH.sub.3                                                                            CF.sub.3                                                                             149-150                       86-a     C.sub.3 H.sub.7 -n                                                                        H   H    H   N   OC.sub.3 H.sub.7 -n                                                                  CH.sub.3                                                                             176-178                       __________________________________________________________________________

                                      TABLE 14a-2                                  __________________________________________________________________________      ##STR1174##                                                                                                              m.p.                                Compound No.                                                                            R.sup.a1  R.sup.a4                                                                           R.sup.a5                                                                           A   B     D     (°C.)                        __________________________________________________________________________      3-a     CH.sub.3  H   H   CH  OCH.sub.3                                                                            OCH.sub.3                                                                            204-206                             24-a     C.sub.3 H.sub.7 -n                                                                       H   H   CH  OCH.sub.3                                                                            OCH.sub.3                                                                            172-173                             25-a     CH.sub.2 CHCH.sub.2                                                                      H   H   CH  OCH.sub.3                                                                            OCH.sub.3                                                                            177-178                             26-a     CH.sub.2 CCH                                                                             H   H   CH  OCH.sub.3                                                                            OCH.sub.3                                                                            188-190                             34-a     C.sub.2 H.sub.5                                                                          H   H   CH  OCH.sub.3                                                                            OCH.sub.3                                                                            170-172                             41-a     CH.sub.2 CHCHCH.sub.3                                                                    H   H   CH  OCH.sub.3                                                                            OCH.sub.3                                                                            133-134                             42-a     C.sub.5 H.sub.11 -n                                                                      H   H   CH  OCH.sub.3                                                                            OCH.sub.3                                                                            132-134                             50-a     CH.sub.2 COCH.sub.3                                                                      H   H   CH  OCH.sub.3                                                                            OCH.sub.3                                                                            186-188                             51-a     C.sub.6 H.sub.13 -n                                                                      H   H   CH  OCH.sub.3                                                                            OCH.sub.3                                                                            163-165                             56-a     CH.sub.3  H   CH.sub.3                                                                           CH  OCH.sub.3                                                                            OCH.sub.3                                                                            190-191                             59-a     CH.sub.2 CHCHCl                                                                          H   H   CH  OCH.sub.3                                                                            OCH.sub.3                                                                            155-156                             62-a     CH.sub.2 C(Cl)CH.sub.2                                                                   H   H   CH  OCH.sub.3                                                                            OCH.sub.3                                                                            190-192                             64-a     CH.sub.2 OCH.sub.3                                                                       H   H   CH  OCH.sub.3                                                                            OCH.sub.3                                                                            169-170                             70-a     C.sub.3 H.sub.7 -n                                                                       H   H   CH  OCH.sub.3                                                                            Cl    144-146                             71-a     C.sub.3 H.sub.7 -n                                                                       H   H   CH  OCH.sub.3                                                                            OCHF.sub.2                                                                           144-145                             74-a     C.sub.3 H.sub.7 -n                                                                       H   H   CH  OCH.sub.3                                                                            CH.sub.3                                                                             175-177                             75-a     C.sub.3 H.sub.7 -n                                                                       H   H   CH  CH.sub.3                                                                             CH.sub.3                                                                             166-168                             76-a     C.sub.3 H.sub.7 -n                                                                       H   H   CH  OCHF.sub.2                                                                           OCHF.sub.2                                                                           173-174                             77-a     C.sub.3 H.sub.7 -n                                                                       H   H   CH  CH.sub.3                                                                             Cl    155-158                             78-a     C.sub.3 H.sub.7 -n                                                                       H   H   N   OCH.sub.3                                                                            CH.sub.3                                                                             184-186                             81-a     Ph        H   H   CH  OCH.sub.3                                                                            OCH.sub.3                                                                            178-180                             __________________________________________________________________________

                                      TABLE 14a-3                                  __________________________________________________________________________      ##STR1175##                                                                                                           m.p.                                   Compound No.                                                                            R.sup.a1                                                                            R.sup.a2                                                                           R.sup.a3                                                                           R.sup.a6                                                                           A   B    D    (°C.)                           __________________________________________________________________________     67-a     C.sub.2 H.sub.5                                                                     H   H   CH.sub.3                                                                           CH  OCH.sub.3                                                                           OCH.sub.3                                                                           178-180                                69-a     C.sub.3 H.sub.7 -n                                                                  H   H   CH.sub.3                                                                           CH  OCH.sub.3                                                                           OCH.sub.3                                                                           167-169                                __________________________________________________________________________

EXAMPLE b-1 ##STR1176##

1.55 g (10 mmol) of 2-amino-4,6-dimethoxyprimidine was dissolved in 40 ml of dry tetrahydrofuran, and 1.42 g (10 mmol) of chlorosulfonyl isocyanate was dropwise added at -40° C. The reaction temperature was raised to 0° C., and then the mixture was cooled again to -40° C. Then, 2.58 g (9.5 mmol) of 2-imino-3-n-propylthiadiazol-4-ine hydroiodide suspended in 40 ml of dry tetrahydrofuran containing 2.22 g (22 mmol) of triethylamine, was added thereto. The reaction temperature was raised to room temperature, and the mixture was further stirred at the same temperature for one hour. Then, the solvent was distilled off under reduced pressure, and then water was added to the obtained residue. The mixture was extracted three times with chloroform. The chloroform layer was washed sequentially with water and a saturated sodium chloride aqueous solution and then dried over anhydrous sodium sulfate. Then, the solvent was distilled off under reduced pressure. Obtained crystals were washed with acetonitrile to obtain 2.25 g of desired 1-(3-n-propyl-4-thiadiazoline-2-sulfonylimino)-3-(4,6-dimethoxyprimidin-2-yl)urea. Melting point: 189°-190° C.

The structures and the physical property values of the compounds prepared by the same method as in Example b-1 are presented in Table 14b.

                                      TABLE 14b                                    __________________________________________________________________________      ##STR1177##                                                                                                       m.p.                                       Compound No.                                                                            R.sup.b1 R.sup.b2                                                                           A   B    D    (°C.)                               __________________________________________________________________________     2-b      CH.sub.3 H   CH  OCH.sub.3                                                                           OCH.sub.3                                                                           216-217                                    3-b      CH.sub.2 CHCH.sub.2                                                                     H   CH  OCH.sub.3                                                                           OCH.sub.3                                                                           197-198                                    4-b      CH.sub.2 CCH                                                                            H   CH  OCH.sub.3                                                                           OCH.sub.3                                                                           196-198                                    5-b      CH.sub.2 COCH.sub.3                                                                     H   CH  OCH.sub.3                                                                           OCH.sub.3                                                                           206-208                                    6-b      CH.sub.3 CH.sub.3                                                                           CH  OCH.sub.3                                                                           OCH.sub.3                                                                           203.5-204.5                                __________________________________________________________________________

EXAMPLE c-1 ##STR1178##

1.55 g (10 mmol) of 2-amino-4,6-dimethoxyprimidine was dissolved in 20 ml of dry tetrahydrofuran, and 1.42 g (10 mmol) of chlorosulfonyl isocyanate was dropwise added thereto in a range of -10° C. to -5° C. The reaction temperature was raised to 0° C., and the mixture was stirred for 5 minutes. The reaction mixture was cooled again to -30° C., and 2.72 g (12 mmol) of 2-imino-3-ethoxythiazolidine hydrobromide and 2.43 g (24 mmol) of triethylamine suspended in 10 ml of dry tetrahydrofuran were gradually added thereto. The reaction temperature was raised to room temperature, and the mixture was further stirred at the same temperature for 20 minutes. Then, the solvent was distilled off under reduced pressure, and then water was added to the obtained residue. Precipitated crystals were extracted three times with 100 ml of chloroform, and the extract was washed once with 100 ml of water and dried over anhydrous sodium sulfate. Then, the solvent was distilled off under reduced pressure. Obtained crystals were washed with ethyl ether and acetonitrile to obtain 2.1 g of desired 1-(3-ethoxythiazolidine-2-sulfonylimino)-3-(4,6-dimethoxypridimin-2-yl)urea. Melting point: 175°-176° C.

EXAMPLE c-2 ##STR1179##

0.62 g (4.0 mmol) of 2-amino-4,6-dimethoxyprimidine was dissolved in 30 ml of dry tetrahydrofuran, and 0.57 g (4.0 mmol) of chlorosulfonyl isocyanate was dropwise added at -50° C. The reaction temperature was raised to room temperature, and then the reaction mixture was cooled again to -50° C. Then, 1.2 g (5.0 mmol) of 2-imino-3-n-propoxythiazolidine hydrobromide suspended in 20 ml of dry tetrahydrofuran containing 1.01 g (10.0 mmol) of triethylamine, was added thereto. The reaction temperature was gradually raised to room temperature, and the mixture was further stirred at the same temperature for 10 minutes. Then, the solvent was distilled off under reduced pressure, and then water was added to the obtained residue. The mixture was extracted three times with 50 ml of chloroform. The chloroform layer was washed with a saturated sodium chloride aqueous solution and then dried over anhydrous sodium sulfate. Then, the solvent was distilled off under reduced pressure. To the obtained residue, ethyl ether and a small amount of acetonitrile were added for crystallization. The crystals were collected by filtration to obtain 0.65 g of desired 1-(3-n-propoxythiazolidine-2-sulfonylimino)-3-(4,6-dimethoxypyridimin-2-yl-)urea. Melting point: 173°-175° C.

EXAMPLE c-3 Preparation of 1-(3-n-propoxythiazolidine-2-sulfonylimino)-3-(4,6-dimethoxytriazin-2-yl)urea ##STR1180##

3.76 g (40.0 mmol) of phenol was dissolved in 40 ml of dry tetrahydrofuran, and 5.66 g (40.0 mmol) of chlorosulfonyl isocyanate was dropwise added thereto at -50° C. The reaction temperature was raised to room temperature, and then the reaction mixture was cooled again to -50° C. Then, 10.6 g (44 mmol) of 2-imino-3-n-propoxythiazolidine hydrobromide suspended in 20 ml of dry acetonitrile containing 8.08 g (80 mmol) of triethylamine, was added thereto. The reaction temperature was gradually raised to room temperature, and the mixture was further stirred at the same temperature for 10 minutes. Then, the solvent was distilled off under reduced pressure, and then water was added to the obtained residue. The mixture was extracted three times with 70 ml of chloroform. The chloroform layer was washed with a saturated sodium chloride aqueous solution and then dried over anhydrous sodium sulfate. Then, the solvent was distilled off under reduced pressure. To the obtained residue, ethyl ether and a small amount of acetonitrile were added for crystallization. Then, the crystals were collected by filtration to obtain 14 g of phenyl N-(3-n-propoxythiazolidine-2-sulfonylimino)carbamate. Then, 0.72 g (2.0 mmol) of the obtained carbamate was dissolved in 30 ml of dry dioxane, and 0.23 g (1.5 mmol) of 2-amino-4,6-dimethoxytriazine was added thereto. The mixture was refluxed under heating for 4 hours. The solvent was distilled off under reduced pressure, and ethyl ether and a small amount of acetonitrile were added for crystallization. Then, the crystals were collected by filtration to obtain 0.3 g of desired 1-(3-n-propoxythiazolidine-2-sulfonylimino)-3-(4,6-dimethoxytriazin-2-yl)urea. Melting point: 166°-167° C.

EXAMPLE c-4 ##STR1181##

0.84 g (6 mmol) of 2-amino-4-methyl-6-methoxytriazine was suspended in 20 ml of dry tetrahydrofuran, and 0.85 g (6 mmol) of chlorosulfonyl isocyanate was dropwise added thereto at room temperature. A heat was generated mildly, and the reaction mixture turned to a pale yellow solution. Then, 1.64 g (6 mmol) of 2-imino-3-(3-chloroallyloxy)thiazolidine hydrobromide and 1.43 g (14 mmol) of tritehylamine suspended in 15 ml of dry tetrahydrofuran were gradually added thereto, and the mixture was further stirred at room temperature for 30 minutes. The solvent was distilled off under reduced pressure, and then water was added to the obtained residue. The resulting oily substance was extracted three times with 80 ml of chloroform. The extract solution was washed once with 100 ml of water and dried over anhydrous sodium sulfate. Then, the solvent was distilled off under reduced pressure. Obtained crystals were washed with ethyl ether and acetonitrile to obtain 1.2 g of desired 1-[3-(3-chloroallyloxy)thiazolidine-2-sulfonylimino]-3-(4-methyl-6-methoxytriazin-2-yl)urea. Melting point: 145°-147° C.

EXAMPLE c-5 ##STR1182##

0.78 g (5 mmol) of 2-amino-4,6-dimethoxypyrimidine was dissolved in 10 ml of dry tetrahydrofuran, and 0.71 g (5 mmol) of chlorosulfonyl isocyanate was dropwise added thereto in a range of -20° C. to -15° C. The reaction temperature was raised to 0° C., and the mixture was stirred for 5 minutes. The mixture was cooled again to -20° C., and 0.90 g (5 mmol) of 2-imino-3-methoxy-4-methylthiazol-4-ine hydrochloride and 1.11 g (11 mmol) of triethylamine suspended in 10 ml of dry tetrahydrofuran, was gradually added thereto. The reaction temperature was raised to room temperature, and the mixture was further stirred at the same temperature for 20 minutes. The solvent was distilled off under reduced pressure, and then water was added to the obtained residue. Precipitated crystals were extracted three times with 50 ml of chloroform. The extract solution was washed once with 50 ml of water and dried over anhydrous sodium sulfate. Then, the solvent was distilled off under reduced pressure. Obtained crystals were washed with ethyl ether and acetonitrile to obtain 1.02 g of desired 1-(3-methoxy-4-methyl-4-thiazolidine-2-sulfonylimino)-3-(4,6-dimethoxypyrimidin-2-yl)urea. Melting point: 183°-185° C.

the structures and the physical property values of the compounds prepared by the same methods as in Examples c-1 to c-5 are presented in Tables 14c-1, 14c-2 and 14c-3.

                                      TABLE 14c-1                                  __________________________________________________________________________      ##STR1183##                                                                                                              m.p.                                Compound No.                                                                            R.sup.c1  R.sup.c2                                                                           R.sup.c3                                                                           A   B     D     (°C.)                        __________________________________________________________________________      2-c     C.sub.2 H.sub.5                                                                          H   H   CH  OCH.sub.3                                                                            CH.sub.3                                                                             182-183                              3-c     C.sub.2 H.sub.5                                                                          H   H   N   OCH.sub.3                                                                            CH.sub.3                                                                             155-156                              4-c     C.sub.2 H.sub.5                                                                          H   H   CH  CH.sub.3                                                                             CH.sub.3                                                                             152-153                              5-c     CH(CH.sub.3).sub.2                                                                       H   H   CH  OCH.sub.3                                                                            OCH.sub.3                                                                            175-178                              6-c     CH.sub.3  H   H   CH  OCH.sub.3                                                                            OCH.sub.3                                                                            193-194                              7-c     CH.sub.3  H   H   CH  OCH.sub.3                                                                            CH.sub.3                                                                             183-185                             11-c     CH(CH.sub.3).sub.2                                                                       H   H   CH  OCH.sub.3                                                                            CH.sub.3                                                                             150-152                             13-c     C.sub.3 H.sub.7 -n                                                                       H   H   CH  OCH.sub.3                                                                            CH.sub.3                                                                             161.5-162.5                         14-c     C.sub.3 H.sub.7 -n                                                                       H   H   N   OCH.sub.3                                                                            CH.sub.3                                                                             163-165                             15-c     C.sub.3 H.sub.7 -n                                                                       H   H   CH  CH.sub.3                                                                             CH.sub.3                                                                             145.5-146.5                         16-c     C.sub.4 H.sub.9 -n                                                                       H   H   CH  OCH.sub.3                                                                            OCH.sub.3                                                                            159-160                             17-c     CH.sub.2 CCH                                                                             H   H   CH  OCH.sub.3                                                                            OCH.sub.3                                                                            172-173                             18-c     CH.sub.2 CHCH.sub.2                                                                      H   H   CH  OCH.sub.3                                                                            OCH.sub.3                                                                            175.5-176.5                         19-c     CH.sub.2 CHCH.sub.2                                                                      H   H   CH  OCH.sub.3                                                                            CH.sub.3                                                                             165-166                             20-c     C.sub.3 H.sub.7 -n                                                                       H   H   CH  OCHF.sub.2                                                                           OCHF.sub.2                                                                           118-119                             21-c     CH.sub.2 CHCH.sub.2                                                                      H   H   CH  CH.sub.3                                                                             CH.sub.3                                                                             95-96                               22-c     CH.sub.2 Ph                                                                              H   H   CH  OCH.sub.3                                                                            OCH.sub.3                                                                            159-161                             23-c     C.sub.3 H.sub.7 -n                                                                       H   H   CH  OCHF.sub.2                                                                           CH.sub.3                                                                             151-152                             25-c     C.sub.3 H.sub.7 -n                                                                       H   H   CH  OCHF.sub.2                                                                           Cl    225-226                             26-c     C.sub.2 H.sub.5                                                                          H   H   N   OCH.sub.3                                                                            OCH.sub.3                                                                            159-160                             27-c     C.sub.2 H.sub.5                                                                          H   H   CH  OCHF.sub.2                                                                           CH.sub.3                                                                             148-149                             28-c     C.sub.2 H.sub.5                                                                          H   H   CH  OCHF.sub.2                                                                           OCHF.sub.2                                                                           161-162                             29-c     C.sub.3 H.sub.7 -n                                                                       H   H   CH  OCH.sub.3                                                                            OCHF.sub.2                                                                           75-77                               30-c     C.sub.2 H.sub.5                                                                          H   H   CH  OCH.sub.3                                                                            OCHF.sub.2                                                                           149-151                             31-c     C.sub.2 H.sub.5                                                                          H   H   CH  OCH.sub.3                                                                            Cl    141-143                             32-c     C.sub.3 H.sub.7 -n                                                                       H   H   CH  OCH.sub.3                                                                            Cl    157-158                             33-c     C.sub.2 H.sub.5                                                                          H   H   CH  CH.sub.3                                                                             Cl    163-164                             34-c     C.sub.3 H.sub.7 -n                                                                       H   H   CH  CH.sub.3                                                                             Cl    153-156                             35-c     CH.sub.2 CHCHCl                                                                          H   H   CH  OCH.sub.3                                                                            OCH.sub.3                                                                            184-185                             36-c     CH.sub.2 CHCHCl                                                                          H   H   CH  OCH.sub.3                                                                            CH.sub.3                                                                             168-169                             38-c     CH.sub.2 CH(CH.sub.3).sub.2                                                              H   H   CH  OCH.sub.3                                                                            OCH.sub.3                                                                            175.5-176.5                         39-c     CH.sub.2 CH(CH.sub.3).sub.2                                                              H   H   CH  OCH.sub.3                                                                            CH.sub.3                                                                             151-152                             40-c     CH.sub.2 CH(CH.sub.3).sub.2                                                              H   H   N   OCH.sub.3                                                                            CH.sub.3                                                                             148.5-149.5                         41-c     CH.sub.2 CH(CH.sub.3).sub.2                                                              H   H   N   OCH.sub.3                                                                            OCH.sub.3                                                                            172-173                             43-c     CH.sub.2 CHCHCl                                                                          H   H   CH  CH.sub.3                                                                             CH.sub.3                                                                             164-165                             44-c     CH.sub.2 CHCHCl                                                                          H   H   N   OCH.sub.3                                                                            OCH.sub.3                                                                            158-163                             46-c     C.sub.5 H.sub.11 -n                                                                      H   H   CH  OCH.sub.3                                                                            OCH.sub.3                                                                            121-122                             47-c     CH.sub.2 CH(CH.sub.3).sub.2                                                              H   H   CH  CH.sub.3                                                                             CH.sub.3                                                                             154-155                             48-c     CH.sub.2 CHCHCl                                                                          H   H   CH  OCH.sub.3                                                                            OCHF.sub.2                                                                           142-143                             49-c     CH.sub.2 C(Cl)CH.sub.2                                                                   H   H   CH  OCH.sub.3                                                                            OCH.sub.3                                                                            178-179                             50-c     CH.sub.2 C(Cl)CH.sub.2                                                                   H   H   CH  OCH.sub.3                                                                            CH.sub.3                                                                             159-160                             51-c     CH.sub.2 C(Cl)CH.sub.2                                                                   H   H   N   OCH.sub.3                                                                            CH.sub.3                                                                             157-158                             52-c     CH.sub.2 C(Cl)CH.sub.2                                                                   H   H   N   OCH.sub.3                                                                            OCH.sub.3                                                                            181-182                             53-c     C.sub.3 H.sub.7 -n                                                                       H   H   N   OC.sub.2 H.sub.5                                                                     CH.sub.3                                                                             134-135                             54-c     C.sub.3 H.sub.7 -n                                                                       H   H   N   OCH.sub.3                                                                            C.sub.2 H.sub.5                                                                      143.5-144.5                         55-c     CH.sub.2 CHCHCl                                                                          H   H   N   OC.sub.2 H.sub.5                                                                     CH.sub.3                                                                             131-133                             56-c     CH.sub.2 CHCHCl                                                                          H   H   N   OCH.sub.3                                                                            C.sub.2 H.sub.5                                                                      128-130                             57-c     CH.sub.2 CHCHCl                                                                          H   H   N   OCH.sub.3                                                                            CH.sub.2 Cl                                                                          133-135                             58-c     C.sub.3 H.sub.7 -n                                                                       H   H   N   OCH.sub.3                                                                            CH.sub.2 Cl                                                                          154-155                             59-c     CH.sub.2 CHCHCl                                                                          H   H   CH  OCHF.sub.2                                                                           CH.sub.3                                                                             136-137                             60-c     C.sub.3 H.sub.7 -n                                                                       H   H   CH  CF.sub.3                                                                             Cl    133-134                             61-c     C.sub.2 H.sub.5                                                                          H   H   N   OC.sub.2 H.sub.5                                                                     CH.sub.3                                                                             161-162                             62-c     C.sub.3 H.sub.7 -n                                                                       H   H   N   OCH.sub.3                                                                            C.sub.3 H.sub.7 -n                                                                   157-158                             63-c     C.sub.3 H.sub.7 -n                                                                       H   H   N   OC.sub.3 H.sub.7 -n                                                                  CH.sub.3                                                                             124-125                             64-c     CH.sub.2 CHCHCl                                                                          H   H   CH  CF.sub.3                                                                             Cl    183-186                             65-c     CH.sub.2 CHCHCl                                                                          H   H   N   OCH.sub.3                                                                            C.sub.3 H.sub.7 -n                                                                   114-115                             66-c     CH.sub.2 CHCHCl                                                                          H   H   N   OC.sub.3 H.sub.7 -n                                                                  CH.sub.3                                                                             128-130                             67-c     CH.sub.2 CHCHCl                                                                          H   H   N   OCH.sub.3                                                                            CF.sub.3                                                                             138-140                             68-c     CH.sub.2 C(Cl)CH.sub.2                                                                   H   H   N   OC.sub.2 H.sub.5                                                                     CH.sub.3                                                                             139-140                             69-c     CH.sub.2 C(Cl)CH.sub.2                                                                   H   H   N   OCH.sub.3                                                                            C.sub.2 H.sub.5                                                                      149-150                             70-c     CH.sub.2 C(Cl)CH.sub.2                                                                   H   H   N   OCH.sub.3                                                                            CF.sub.3                                                                             152-154                             71-c     CH.sub.2 C(Cl)CH.sub.2                                                                   H   H   CH  OCH.sub.3                                                                            OCHF.sub.2                                                                           86-87                               __________________________________________________________________________

                                      TABLE 14c-2                                  __________________________________________________________________________      ##STR1184##                                                                                                          m.p.                                    Compound No.                                                                            R.sup.c1                                                                           R.sup.c4                                                                           R.sup.c5                                                                           R.sup.c6                                                                           A   B    D    (°C.)                            __________________________________________________________________________      8-c     C.sub.2 H.sub.5                                                                    H   H   H   CH  OCH.sub.3                                                                           OCH.sub.3                                                                           189-190                                  9-c     C.sub.2 H.sub.5                                                                    H   H   H   CH  OCH.sub.3                                                                           CH.sub.3                                                                            165-166                                 10-c     C.sub.2 H.sub.5                                                                    H   H   H   CH  CH.sub.3                                                                            CH.sub.3                                                                            178-179                                 __________________________________________________________________________

                  TABLE 14c-3                                                      ______________________________________                                          ##STR1185##                                                                   Com-                                                                           pound                                     m.p.                                 No.   R.sup.c1                                                                              R.sup.c7                                                                              R.sup.c8                                                                            A    B     D     (°C.)                         ______________________________________                                         42-c  CH.sub.3                                                                              CH.sub.3                                                                              CH.sub.3                                                                            CH   OCH.sub.3                                                                            OCH.sub.3                                                                            180-192                                                                        (decomposed)                         ______________________________________                                    

EXAMPLE d-1 ##STR1186##

1.55 g (10 mmol) of 2-amino-4,6-dimethoxypyrimidine was dissolved in 30 ml of dry tetrahydrofuran, and 1.42 g (10 mmol) of chlorosulfonyl isocyanate was dropwise added thereto in a range of from -20° C. to -15° C. The reaction temperature was raised to 0° C., and the mixture was further stirred at the same temperature for 10 minutes. The reaction mixture was cooled again to -30° C., and a mixture comprising 2.84 g (11 mmol) of 3-methyl-2-iminothiazolidin-4-one hydroiodide, 2.22 g (22 mmol) of triethylamine and 30 ml of dry tetrahydrofuran, was added thereto. The reaction temperature was raised to room temperature, and the mixture was further stirred at the same temperature for 20 minutes. Then, the solvent was distilled off under reduced pressure, and then 100 ml of water was added to the obtained residue. Precipitated crystals were extracted three times with 100 ml of chloroform. The chloroform layer was washed with water and then dried over anhydrous sodium sulfate. Then, the solvent was distilled off under reduced pressure. Obtained crystals were washed with a solvent mixture of ethyl ether/acetonitrile and collected by filtration to obtain 1.5 g of desired 1-(3-methylthiazolidin-4-one-2-sulfonylimiono)-3-(4,6-dimethoxypyrimidin-2-yl)urea as colorless crystals. Melting point: 200°-201° C.

EXAMPLE d-2 ##STR1187##

1.16 g (7.5 mmol) of 2-amino-4,6-dimethoxypyrimidine was dissolved in 20 ml of dry tetrahydrofuran, and 1.07 g (7.5 mmol) of chlorosulfonyl isocyanate was dropwise added thereto at -40° C. The reaction temperature was raised to 0° C., and then the reaction mixture was cooled again to -40° C. Then, a mixture comprising 1.16 g (7.5 mmol) of 1-methyl-3-n-propyl-2-iminoimidazolidin-4-one, 0.83 g (8.2 mmol) of triethylamine and 20 ml of dry tetrahydrofuran, was added thereto. The reaction temperature was raised to room temperature, and the mixture was further stirred at the same temperature for 2 hours. Then, the solvent was distilled off under reduced pressure, and then 100 ml of water was added to the obtained residue. The mixture was extracted three times with 100 ml of chloroform. Then, the chloroform layer was washed with water and then dried over anhydrous sodium sulfate. The solvent was distilled off under reduced pressure, and precipitated crystals were washed with a solvent mixture of ethyl ether/acetonitrile and collected by filtration to obtain 0.16 g of desired 1-(1-methyl-3-n-propylimidazolidin-4-one-2-sulfonylimino)-3-(4,6-dimethoxyprimidin-2-yl)urea. Melting point: 96°-98° C.

The structures and the physical property values of the compounds prepared by the same methods as in Examples d-1 and d-2 are presented in Table 14d.

                                      TABLE 14d                                    __________________________________________________________________________      ##STR1188##                                                                                                           m.p.                                   Compound No.                                                                            R.sup.d1 R.sup.d4                                                                           R.sup.d5                                                                           A   B    D    (°C.)                           __________________________________________________________________________     3-d      CH.sub.3 H   CH.sub.3                                                                           CH  OCH.sub.3                                                                           OCH.sub.3                                                                           188-189                                4-d      C.sub.2 H.sub.5                                                                         H   CH.sub.3                                                                           CH  OCH.sub.3                                                                           OCH.sub.3                                                                           111-113                                5-d      CH.sub.2 CHCH.sub.2                                                                     H   CH.sub.3                                                                           CH  OCH.sub.3                                                                           OCH.sub.3                                                                           156-158                                6-d      CH.sub.2 CCH                                                                            H   CH.sub.3                                                                           CH  OCH.sub.3                                                                           OCH.sub.3                                                                           181-182                                7-d      CH.sub.2 COCH.sub.3                                                                     H   CH.sub.3                                                                           CH  OCH.sub.3                                                                           OCH.sub.3                                                                           190-192                                8-d      CH.sub.2 CO.sub.2 CH.sub.3                                                              H   CH.sub.3                                                                           CH  OCH.sub.3                                                                           OCH.sub.3                                                                           188-190                                9-d      CH.sub.2 OCH.sub.3                                                                      H   CH.sub.3                                                                           CH  OCH.sub.3                                                                           OCH.sub.3                                                                           155-156                                10-d     CH.sub.2 SCH.sub.3                                                                      H   CH.sub.3                                                                           CH  OCH.sub.3                                                                           OCH.sub.3                                                                           115-120                                                                        (decomposed)                           __________________________________________________________________________

EXAMPLE e-1 ##STR1189##

0.32 g (2.06 mmol) of 2-amino-4,6-dimethoxypyrimidine was dissolved in 40 ml of dry tetrahydrofuran, and the solution was cooled to -40° C. At the same temperature, 0.29 g (2.05 mmol) of chlorosulfonyl isocyanate was dropwise added thereto. Then, the temperature was raised to 0° C. The mixture was cooled again to -40° C., and then a mixed solution comprising 0.4 g (2.56 mmol) of 3,6-dihydro-3-n-propyl-2H-1,3-thiazin-2-imine, 0.26 g (2.57 mmol) of triethylamine and 40 ml of dry tetrahydrofuran, was dropwise added thereto. The mixture was gradually heated to room temperature with stirring, and then the solvent was distilled off under reduced pressure. 100 ml of water was added to the residue, and then the mixture was extracted twice with 50 ml of chloroform. The chloroform layer was washed with water and then dried over anhydrous sodium sulfate. Then, chloroform was distilled off under reduced pressure. Obtained crystals were washed with acetonitrile and then with ethyl ether to obtain 0.3 g of desired 1-(3,6-dihydro-3-n-propyl-2H-1,3-thiazine-2-sulfonylimino)-3-(4,6-dimethoxyprimidin-2-yl)urea. Melting point: 161°-163° C.

EXAMPLE e-2 ##STR1190##

1.55 g (10 mmol) of 2-amino-4,6-dimethoxypyrimidine was dissolved in 30 ml of dry tetrahydrofuran, and 1.42 g (10 mmol) of chlorosulfonyl isocyanate was dropwise added thereto in a range of from -15° C. to -5° C. The reaction solution was heated to 0° C. and then further stirred at the same temperature for 15 minutes. Then, the reaction solution was cooled again to -30° C., and a mixed solution comprising 1.56 g (12 mmol) of 3,4,5,6-tetrahydro-3-methyl-2H-1,3-thiazin-2-imine, 1.21 g (12 mmol) of triethylamine and 10 ml of dry tetrahydrofuran, was dropwise added thereto. The reaction solution was gradually heated to room temperature with stirring, and then the solvent was distilled off under reduced pressure. 80 ml of water was added to the residue, and precipitated crystals were extracted three times with 60 ml of chloroform. The chloroform layer was washed with water and dried over anhydrous sodium sulfate. Then, chloroform was distilled off under reduced pressure.

Obtained crystals were washed with a solvent mixture of ethyl ether/acetonitrile to obtain 1.2 g of desired 1-(3,4,5,6-tetrahydro-3-methyl-2H-1,3-thiazine-2-sulfonylimino)-3-(4,6-dimethoxypyrimidin-2-yl)urea. Melting point 188°-190° C.

The structures and the physical property values of the compounds prepared by the same methods as in Examples e-1 and e-2 are presented in Tables 14e-1 and 14e-2.

                                      TABLE 14e-1                                  __________________________________________________________________________      ##STR1191##                                                                                                             m.p.                                 Compound No.                                                                            R.sup.e1                                                                              R.sup.e2                                                                           R.sup.e3                                                                           R.sup.e4                                                                           A   B    D    (°C.)                         __________________________________________________________________________     3-e      CH.sub.3                                                                              H   H   H   CH  OCH.sub.3                                                                           OCH.sub.3                                                                           194-196                              4-e      CH.sub.2 OCH.sub.3                                                                    H   H   H   CH  OCH.sub.3                                                                           OCH.sub.3                                                                           158-160                              __________________________________________________________________________

                                      TABLE 14e-2                                  __________________________________________________________________________      ##STR1192##                                                                                                           m.p.                                   Compound No.                                                                            R.sup.e1                                                                            R.sup.e8                                                                           R.sup.e9                                                                           R.sup.e10                                                                          A   B    D    (°C.)                           __________________________________________________________________________     5-e      C.sub.3 H.sub.7 -n                                                                  H   H   H   CH  OCH.sub.3                                                                           OCH.sub.3                                                                           166-167                                __________________________________________________________________________

EXAMPLE f-1 ##STR1193##

1.55 g (10 mmol) of 2-amino-4,6-dimethoxypyrimidine was dissolved in 30 ml of dry tetrahydrofuran, and 1.42 g (10 mmol) of chlorosulfonyl isocyanate was dropwise added thereto at -20° C. The reaction temperature was raised to -5° C., and the mixture was stirred at the same temperature for 5 minutes. The reaction mixture was cooled again to -20° C., and a mixture comprising 2.28 g (10 mmol) of 2-imino-3-methyloxazolidine hydroiodide, 2.22 g (22 mmol) of triethylamine and 30 ml of dry tetrahydrofuran, was added thereto. The reaction temperature was raised to room temperature, and the mixture was further stirred at the same temperature for one hour. Then, the solvent was distilled off under reduced pressure, and then 100 ml of water was added to the obtained residue. Precipitated crystals were collected by filtration, washed with water and then with a solvent mixture of ethyl ether/acetonitrile and dried to obtain 0.8 g of desired 1-(3-methloxazolidine-2-sulfonylimino)-3-(4,6-dimethoxypyrimidin-2-yl)urea. Melting point: 174°-175° C.

The structures and the physical property values of the compounds prepared by the same method as in Example f-1 are presented in Tables 14f.

                                      TABLE 14f                                    __________________________________________________________________________      ##STR1194##                                                                                                           m.p.                                   Compound No.                                                                            R.sup.f1 R.sup.f5                                                                           R.sup.f6                                                                           A   B    D    (°C.)                           __________________________________________________________________________     2-f      CH.sub.2 CHCH.sub.2                                                                     H   H   CH  OCH.sub.3                                                                           OCH.sub.3                                                                           157-159                                __________________________________________________________________________

EXAMPLE q-1 ##STR1195##

1.55 g (10 mmol) of 2-amino-4,6-dimethoxypyrimidine was dissolved in 40 ml of dry tetrahydrofuran, and 1.42 g (10 mmol) of chlorosulfonyl isocyanate was dropwise added thereto in a range of from -20° C. to -15° C. The reaction temperature was raised to 0° C., and the mixture was cooled again to -20° C. Then, a mixture comprising 2.5 g (10.2 mmol) of N,N-dimethyl-S-methylisothiourea hydroiodide, 2.22 g (22 mmol) of triethylamine and 30 ml of dry tetrahydrofuran, was added thereto. The reaction temperature was raised to room temperature, and the mixture was further stirred at the same temperature for 10 minutes. Then, the solvent was distilled off under reduced pressure, and then 80 ml of water was added to the obtained residue. The mixture was extracted three times with 30 ml of chloroform. The chloroform layer was washed with water and then dried over anhydrous sodium sulfate. Then, solvent was distilled off under reduced pressure. Obtained crystals were washed with a solvent mixture of ethyl ether/ acetonitrile to obtain 2 g of desired 1-[N-((methylthio-N,N-dimethylamino)methylene)aminosulfonyl]-3-(4,6-dimethoxypyrimidin-2-yl)urea. Melting point: 167°-168° C.

EXAMPLE g-2 ##STR1196##

1.55 g (10 mmol) of 2-amino-4,6-dimethoxypyrimidine was dissolved in 40 ml of dry tetrahydrofuran, and 1.42 g (10 mmol) of chlorosulfonyl isocyanate was dropwise added thereto in a range of from -20° C. to -15° C. The reaction temperature was raised to 0° C., and the mixture was cooled again to -20° C. Then, a mixture comprising 2.60 g (10 mmol) of N-ethyl-N-methyl-S-methylisothiourea hydroiodide, 2.22 g (22 mmol) of triethylamine and 30 ml of dry tetrahydrofuran, was added thereto. The reaction temperature was raised to room temperture, and the mixture was further stirred at the same temperature for one hour. Then, the solvent was distilled off under reduced pressure, and 80 ml of water was added to the obtained residue. The mixture was extracted three times with 50 ml of chloroform. The chloroform layer was washed with water, and then dried over anhydrous sodium sulfate. Then, the solvent was distilled off under reduced pressure. Obtained crystals were washed with acetonitrile to obtain 1.32 g of desired 1-[N-((methylthio-N-ethyl-N-methylamino)methylene)aminosulfonyl]-3-(4,6-dimethoxypyrimidin-2-yl)urea. Melting point: 143°-144° C.

EXAMPLE q-3 ##STR1197##

0.78 g (5 mmol) of 2-amino-4,6-dimethoxypyrimidine was dissolved in 20 ml of dry tetrahydrofuran, and 0.71 g (5 mmol) of chlorosulfonyl isocyanate was dropwise added thereto in a range of from -20° C. to -15° C. The reaction temperature was raised to 0° C., and then the mixture was cooled again to -20° C. Then, a mixture comprising 1.31 g (5 mmol) of N-methoxy-N-methyl-S-methylisothiourea hydroiodide, 1.11 g (11 mmol) of triethylamine and 15 ml of dry tetrahydrofuran, was added thereto. The reaction temperature was raised to room temperature, and the mixture was further stirred at the same temperature for one hour. Then, the solvent was distilled off under reduced pressure, and then 40 ml of water was added to the obtained residue. The mixture was extracted three times with 25 ml of chloroform. The chloroform layer was washed with water, and then dried over anhydrous sodium sulfate. Then, the solvent was distilled off under reduced pressure. Obtained crystals were washed with acetonitrile to obtain 1.51 g of desired 1-[N-((methylthio-N-methoxy-N-methylamino)methylene)aminosulfonyl]-3-(4,6-dimethoxypyrimidin-2-yl)urea. Melting point: 165°-167° C.

The structures and the physical property values of the compounds prepared by the same methods as in Examples g-1 to g-3 are presented in Table 14g.

                                      TABLE 14g                                    __________________________________________________________________________      ##STR1198##                                                                                                                m.p.                              Compound No.                                                                            R.sup.g1 R.sup.g2                                                                           R.sup.g3 A   B    D    (°C.)                      __________________________________________________________________________      2-g     C.sub.2 H.sub.5                                                                         CH.sub.3                                                                           CH.sub.3 CH  OCH.sub.3                                                                           OCH.sub.3                                                                           129-130                            3-g     C.sub.3 H.sub.7 -n                                                                      CH.sub.3                                                                           CH.sub.3 CH  OCH.sub.3                                                                           OCH.sub.3                                                                           115-116                            4-g     CH.sub.2 CHCH.sub.2                                                                     CH.sub.3                                                                           CH.sub.3 CH  OCH.sub.3                                                                           OCH.sub.3                                                                           131-132                            5-g     CH.sub.2 CCH                                                                            CH.sub.3                                                                           CH.sub.3 CH  OCH.sub.3                                                                           OCH.sub.3                                                                           140-141                            6-g     CH.sub.3 CH.sub.3                                                                           COCH.sub.3                                                                              CH  OCH.sub.3                                                                           OCH.sub.3                                                                           162-164                            8-g     CH.sub.3 (CH.sub.2).sub.4                                                                            CH  OCH.sub.3                                                                           OCH.sub.3                                                                           184-186                            9-g     CH.sub.3 CH.sub.3                                                                           C.sub.3 H.sub.7 -n                                                                      CH  OCH.sub.3                                                                           OCH.sub.3                                                                           123-125                           10-g     CH.sub.3 CH.sub.3                                                                           Ph       CH  OCH.sub.3                                                                           OCH.sub.3                                                                           163-164                           11-g     CH.sub.3 CH.sub.3                                                                           CH.sub.3 CH  OCH.sub.3                                                                           CH.sub.3                                                                            178-179                           13-g     CH.sub.3 CH.sub.3                                                                           OC.sub.2 H.sub.5                                                                        CH  OCH.sub.3                                                                           OCH.sub.3                                                                           142-143                           14-g     CH.sub.3 CH.sub.3                                                                           OC.sub.3 H.sub.7 -n                                                                     CH  OCH.sub.3                                                                           OCH.sub.3                                                                           124-125                           15-g     CH.sub.3 CH.sub.3                                                                           OC.sub.3 H.sub.7 -n                                                                     CH  OCH.sub.3                                                                           CH.sub.3                                                                            142-143                           16-g     CH.sub.3 CH.sub.3                                                                           OC.sub.2 H.sub.5                                                                        CH  OCH.sub.3                                                                           CH.sub.3                                                                            141-142                           17-g     CH.sub.3 CH.sub.3                                                                           OC.sub.2 H.sub.5                                                                        N   OCH.sub.3                                                                           CH.sub.3                                                                            148-149                           18-g     CH.sub.3 CH.sub.3                                                                           OC.sub.3 H.sub.7 -n                                                                     N   OCH.sub.3                                                                           CH.sub.3                                                                            138-139                           19-g     CH.sub.3 CH.sub.3                                                                           CH.sub.2 CHCH.sub.2                                                                     CH  OCH.sub.3                                                                           OCH.sub.3                                                                           138-141                           20-g     CH.sub.3 CH.sub.3                                                                           CH.sub.3 N   OCH.sub.3                                                                           CH.sub.3                                                                            166-167                           __________________________________________________________________________

Now, Formulation Examples of the herbicides containing the compounds of the present invention will be given specifically. However, it should be understood that the present invention is by no means restricted to such specific Examples. In the following Formulation Examples, "parts" means "parts by weight".

    ______________________________________                                         Wettable powder                                                                ______________________________________                                         Compound of the present invention                                                                      5-80    parts                                          Solid carrier           10-85   parts                                          Surfactant              1-10    parts                                          Other                   1-5     parts                                          ______________________________________                                    

As other, a coagulation preventing agent may, for example, be mentioned.

    ______________________________________                                         Emulsifiable concentrate                                                       Compound of the present invention                                                                      1-30    parts                                          Liquid carrier          30-95   parts                                          Surfactant              5-15    parts                                          Flowable                                                                       Compound of the present invention                                                                      5-70    parts                                          Liquid carrier          15-65   parts                                          Surfactant              5-12    parts                                          Other                   5-30    parts                                          ______________________________________                                    

As other, an antifreezing agent and a thickener may, for example, be mentioned.

    ______________________________________                                         Granular wettable powder (dry flowable)                                        Compound of the present invention                                                                        20-90   parts                                        Solid carrier             10-60   parts                                        Surfactant                1-20    parts                                        Granule                                                                        Compound of the present invention                                                                        0.1-10  parts                                        Solid carrier             90-99.9 parts                                        Other                     1-5     parts                                        FORMULATION EXAMPLE a-1: Wettable                                              powder                                                                         Compound No. 1-a of the present invention                                                                20      parts                                        Zeeklite A (tradename for a kaolin-type                                                                  76      parts                                        clay, manufactured by Zeeklite Industries,                                     Co., Ltd.)                                                                     Sorpol 5039 (tradename for a mixture of a                                                                2       parts                                        nonionic surfactant and an anionic                                             surfactant, manufactured by Toho Chemical                                      Industry Co., Ltd.)                                                            Carplex (tradename for a coagulation-                                                                    2       parts                                        preventing agent composed of a white carbon,                                   manufactured by Shionogi Pharmaceutical                                        Co., Ltd.)                                                                     ______________________________________                                    

The above ingredients are homogeneously pulverized and mixed to form a wettable powder.

    ______________________________________                                         FORMULATION EXAMPLE a-2: Wettable powder                                       ______________________________________                                         Compound No. 2-a of the present invention                                                                  40    parts                                        Zeeklite A (tradename for a kaolin-type                                                                    54    parts                                        clay, manufactured by Zeeklite Industries,                                     Co., Ltd.)                                                                     Sorpol 5039 (tradename for a mixture of a                                                                  2     parts                                        nonionic surfactant and an anionic                                             surfactant, manufactured by Toho Chemical                                      Industry Co., Ltd.)                                                            Carplex (tradename for a coagulation-                                                                      4     parts                                        preventing agent composed of a white carbon,                                   manufactured by Shionogi Pharmaceutical                                        Co., Ltd.)                                                                     ______________________________________                                    

The above ingredients are homogeneously pulverized and mixed to form a wettable powder.

    ______________________________________                                         FORMULATION EXAMPLE a-3: Emulsifiable                                          concentrate                                                                    ______________________________________                                         Compound No. 3-a of the present invention                                                                 5      parts                                        Xylene                     75     parts                                        N,N-dimethylformamide      15     parts                                        Sorpol 2680 (tradename for a mixture of a                                                                 5      parts                                        nonionic surfactant and an anionic                                             surfactant, manufactured by Toho Chemical                                      Industry Co., Ltd.)                                                            ______________________________________                                    

The above ingredients are homogeneously mixed to form an emulsifiable concentrate.

    ______________________________________                                         FORMULATION EXAMPLE a-4: Flowable                                              ______________________________________                                         Compound No. 7-a of the present invention                                                                25     parts                                         Agrizole S-710 (tradename for a nonionic                                                                 10     parts                                         surfactant, manufactured by Kao Corp.)                                         Runox 1000C (tradename for an anionic                                                                    0.5    part                                          surfactant, manufactured by Toho Chemical                                      Industry Co., Ltd.)                                                            1% Rodopol water (tradename for a thickener,                                                             20     parts                                         manufactured by Rhone-Poulenc)                                                 Water                     44.5   parts                                         ______________________________________                                    

The above ingredients were homogeneously mixed to obtain a flowable.

    ______________________________________                                         FORMULATION EXAMPLE a-5: Flowable                                              ______________________________________                                         Compound No. 8-a of the present invention                                                                40     parts                                         Agrizole S-710 (tradename for a nonionic                                                                 10     parts                                         surfactant, manufactured by Kao Corp.)                                         Runox 1000C (tradename for an anionic                                                                    0.5    part                                          surfactant, manufactured by Toho Chemical                                      Industry Co., Ltd.)                                                            1% Rodopol water (tradename for a thickener,                                                             20     parts                                         manufactured by Rhone-Poulenc)                                                 Water                     29.5   parts                                         ______________________________________                                    

The above ingredients were homogeneously mixed to obtain a flowable.

    ______________________________________                                         FORMULATION EXAMPLE a-6: Granular wettable                                     powder (dry flowable)                                                          ______________________________________                                         Compound No. 10-a of the present invention                                                                 75    parts                                        Isoban No. 1 (tradename for an anionic                                                                     10    parts                                        surfactant, manufactured by Kuraray Isoprene                                   Chemical Co., Ltd.)                                                            Vanirex N (tradename for an anionic                                                                        5     parts                                        surfactant, manufactured by Sanyo Kokusaku                                     Pulp Co., Ltd.)                                                                Carplex #80 (tradename for a white carbon,                                                                 10    parts                                        manufactured by Shionogi Pharmaceutical                                        Co., Ltd.)                                                                     ______________________________________                                    

The above ingredients are uniformly mixed and pulverized to form a dry flowable.

    ______________________________________                                         FORMULATION EXAMPLE a-7; Granule                                               ______________________________________                                         Compound No. 69-a of the present invention                                                               1     part                                           Bentonite                 55    parts                                          Talc                      44    parts                                          ______________________________________                                    

The above ingredients were homogeneously mixed and pulverized, and after an addition of a small amount of water, the mixture was stirred, mixed and granulated by an extrusion-type granulating machine, followed by drying to obtain a granule.

    ______________________________________                                         FORMULATION EXAMPLE b-1: Wettable powder                                       ______________________________________                                         Compound No. 1-b of the present invention                                                                  20    parts                                        Zeeklite A (tradename for a kaolin-type                                                                    76    parts                                        clay, manufactured by Zeeklite Industries,                                     Co., Ltd.)                                                                     Sorpol 5039 (tradename for a mixture of a                                                                  2     parts                                        nonionic surfactant and an anionic                                             surfactant, manufactured by Toho Chemical                                      Industry Co., Ltd.)                                                            Carplex (tradename for a coagulation-                                                                      2     parts                                        preventing agent composed of a white carbon,                                   manufactured by Shionogi Pharmaceutical                                        Co., Ltd.)                                                                     ______________________________________                                    

The above ingredients are homogeneously pulverized and mixed to form a wettable powder.

    ______________________________________                                         FORMULATION EXAMPLE b-2: Wettable powder                                       ______________________________________                                         Compound No. 2-b of the present invention                                                                  40    parts                                        Zeeklite A (tradename for a kaolin-type                                                                    54    parts                                        clay, manufactured by Zeeklite Industries,                                     Co., Ltd.)                                                                     Sorpol 5039 (tradename for a mixture of a                                                                  2     parts                                        nonionic surfactant and an anionic                                             surfactant, manufactured by Toho Chemical                                      Industry Co., Ltd.)                                                            Carplex (tradename for a coagulation-                                                                      4     parts                                        preventing agent composed of a white carbon,                                   manufactured by Shionogi Pharmaceutical                                        Co., Ltd.)                                                                     ______________________________________                                    

The above ingredients are homogeneously pulverized and mixed to form a wettable powder.

    ______________________________________                                         FORMULATION EXAMPLE b-3: Emulsifiable                                          concentrate                                                                    ______________________________________                                         Compound No. 3-b of the present invention                                                                  5     parts                                        Xylene                      75    parts                                        N,N-dimethylformamide       15    parts                                        Sorpol 2680 (tradename for a mixture of a                                                                  5     parts                                        nonionic surfactant and an anionic                                             surfactant, manufactured by Toho Chemical                                      Industry Co., Ltd.)                                                            ______________________________________                                    

The above ingredients are homogeneously mixed to form an emulsifiable concentrate.

    ______________________________________                                         FORMULATION EXAMPLE b-4: Flowable                                              ______________________________________                                         Compound No. 1-b of the present invention                                                                25     parts                                         Agrizole S-710 (tradename for a nonionic                                                                 10     parts                                         surfactant, manufactured by Kao Corp.)                                         Runox 1000C (tradename for an anionic                                                                    0.5    part                                          surfactant, manufactured by Toho Chemical                                      Industry Co., Ltd.)                                                            1% Rodopol water (tradename for a thickener,                                                             20     parts                                         manufactured by Rhone-Poulenc)                                                 Water                     44.5   parts                                         ______________________________________                                    

The above ingredients were homogeneously mixed to obtain a flowable.

    ______________________________________                                         FORMULATION EXAMPLE b-5: Flowable                                              ______________________________________                                         Compound No. 4-b of the present invention                                                                40     parts                                         Agrizole S-710 (tradename for a nonionic                                                                 10     parts                                         surfactant, manufactured by Kao Corp.)                                         Runox 1000C (tradename for an anionic                                                                    0.5    part                                          surfactant, manufactured by Toho Chemical                                      Industry Co., Ltd.)                                                            1% Rodopol water (tradename for a thickener,                                                             20     parts                                         manufactured by Rhone-Poulenc)                                                 Water                     29.5   parts                                         ______________________________________                                    

The above ingredients were homogeneously mixed to obtain a flowable.

    ______________________________________                                         FORMULATION EXAMPLE b-6: Granular wettable                                     powder (dry flowable)                                                          ______________________________________                                         Compound No. 5-b of the present invention                                                                  75    parts                                        Isoban No. 1 (tradename for an anionic                                                                     10    parts                                        surfactant, manufactured by Kuraray Isoprene                                   Chemical Co., Ltd.)                                                            Vanirex N (tradename for an anionic                                                                        5     parts                                        surfactant, manufactured by Sanyo Kokusaku                                     Pulp Co., Ltd.)                                                                Carplex #80 (tradename for a white carbon,                                                                 10    parts                                        manufactured by Shionogi Pharmaceutical                                        Co., Ltd.)                                                                     ______________________________________                                    

The above ingredients are uniformly mixed and pulverized to form a dry flowable.

    ______________________________________                                         FORMULATION EXAMPLE b-7: Granule                                               ______________________________________                                         Compound No. 6-b of the present invention                                                                1     part                                           Bentonite                 55    parts                                          Talc                      44    parts                                          ______________________________________                                    

The above ingredients were homogeneously mixed and pulverized, and after an addition of a small amount of water, the mixture was stirred, mixed and granulated by an extrusion-type granulating machine, followed by drying to obtain a granule.

    ______________________________________                                         FORMULATION EXAMPLE c-1: Wettable powder                                       ______________________________________                                         Compound No. 1-c of the present invention                                                                  20    parts                                        Zeeklite A (tradename for a kaolin-type                                                                    76    parts                                        clay, manufactured by Zeeklite Industries,                                     Co.,Ltd.)                                                                      Sorpol 5039 (tradename for a mixture of a                                                                  2     parts                                        nonionic surfactant and an anionic                                             surfactant, manufactured by Toho Chemical                                      industry Co., Ltd.)                                                            Carplex (tradename for a coagulation-                                                                      2     parts                                        preventing agent composed of a white carbon,                                   manufactured by Shionogi Pharmaceutical                                        Co., Ltd.)                                                                     ______________________________________                                    

The above ingredients are homogeneously pulverized and mixed to form a wettable powder.

    ______________________________________                                         FORMULATION EXAMPLE c-2: Wettable powder                                       ______________________________________                                         Compound No. 2-c of the present invention                                                                  40    parts                                        Zeeklite A (tradename for a kaolin-type                                                                    54    parts                                        clay, manufactured by Zeeklite Industries,                                     Co., Ltd.)                                                                     Sorpol 5039 (tradename for a mixture of a                                                                  2     parts                                        nonionic surfactant and an anionic                                             surfactant, manufactured by Toho Chemical                                      Industry Co., Ltd.)                                                            Carplex (tradename for a coagulation-                                                                      4     parts                                        preventing agent composed of a white carbon,                                   manufactured by Shionogi Pharmaceutical                                        Co., Ltd.)                                                                     ______________________________________                                    

The above ingredients are homogeneously pulverized and mixed to form a wettable powder.

    ______________________________________                                         FORMULATION EXAMPLE c-3: Emulsifiable                                          concentrate                                                                    ______________________________________                                         Compound No. 12-c of the present invention                                                                 5     parts                                        Xylene                      75    parts                                        N,N-dimethylformamide       15    parts                                        Sorpol 2680 (tradename for a mixture of a                                                                  5     parts                                        nonionic surfactant and an anionic                                             surfactant, manufactured by Toho Chemical                                      Industry Co., Ltd.)                                                            ______________________________________                                    

The above ingredients are homogeneously mixed to form an emulsifiable concentrate.

    ______________________________________                                         FORMULATION EXAMPLE c-4: Flowable                                              ______________________________________                                         Compound No. 24-c of the present invention                                                               25     parts                                         Agrizole S-710 (tradename for a nonionic                                                                 10     parts                                         surfactant, manufactured by Kao Corp.)                                         Runox 1000C (tradename for an anionic                                                                    0.5    part                                          surfactant, manufactured by Toho Chemical                                      Industry Co., Ltd.)                                                            1% Rodopol water (tradename for a thickener,                                                             20     parts                                         manufactured by Rhone-Poulenc)                                                 Water                     44.5   parts                                         ______________________________________                                    

The above ingredients were homogeneously mixed to obtain a flowable.

    ______________________________________                                         FORMULATION EXAMPLE c-5: Flowable                                              ______________________________________                                         Compound No. 37-c of the present invention                                                               40     parts                                         Agrizole S-710 (tradename for a nonionic                                                                 10     parts                                         surfactant, manufactured by Kao Corp.)                                         Runox 1000C (tradename for an anionic                                                                    0.5    part                                          surfactant, manufactured by Toho Chemical                                      Industry Co., Ltd.)                                                            1% Rodopol water (tradename for a thickener,                                                             20     parts                                         manufactured by Rhone-Poulenc)                                                 Water                     29.5   parts                                         ______________________________________                                    

The above ingredients were homogeneously mixed to obtain a flowable.

    ______________________________________                                         FORMULATION EXAMPLE c-6: Granular wettable powder                              (dry flowable)                                                                 ______________________________________                                         Compound No. 45-c of the present invention                                                                75    parts                                         Isoban No. 1 (tradename for an anionic                                                                    10    parts                                         surfactant, manufactured by Kuraray Isoprene                                   Chemical Co., Ltd.)                                                            Vanirex N (tradename for an anionic                                                                       5     parts                                         surfactant, manufactured by Sanyo Kokusaku                                     Pulp Co., Ltd.)                                                                Carplex #80 (tradename for a white carbon,                                                                10    parts                                         manufactured by Shionogi Pharmaceutical Co., Ltd.)                             ______________________________________                                    

The above ingredients are uniformly mixed and pulverized to form a dry flowable.

    ______________________________________                                         FORMULATION EXAMPLE c-7: Granule                                               ______________________________________                                         Compound No. 48-c of the present invention                                                                1     part                                          Bentonite                  55    parts                                         Talc                       44    parts                                         ______________________________________                                    

The above ingredients were homogeneously mixed and pulverized, and after an addition of a small amount of water, the mixture was stirred, mixed and granulated by an extrusion-type granulating machine, followed by drying to obtain a granule.

    ______________________________________                                         FORMULATION EXAMPLE d-1: Wettable powder                                       ______________________________________                                         Compound No. 1-d of the present invention                                                                 20    parts                                         Zeeklite A (tradename for a kaolin-type                                                                   76    parts                                         clay, manufactured by Zeeklite Industries, Co., Ltd.)                          Sorpol 5039 (tradename for a mixture of a                                                                 2     parts                                         nonionic surfactant and an anionic                                             surfactant, manufactured by Toho Chemical                                      Industry Co., Ltd.)                                                            Carplex (tradename for a coagulation-                                                                     2     parts                                         preventing agent composed of a white carbon                                    manufactured by Shionogi Pharmaceutical Co., Ltd.)                             ______________________________________                                    

The above ingredients are homogeneously pulverized and mixed to form a wettable powder.

    ______________________________________                                         FORMULATION EXAMPLE d-2: Wettable powder                                       ______________________________________                                         Compound No. 2-d of the present invention                                                                 40    parts                                         Zeeklite A (tradename for a kaolin-type                                                                   54    parts                                         clay, manufactured by Zeeklite Industries, Co., Ltd.)                          Sorpol 5039 (tradename for a mixture of a                                                                 2     parts                                         nonionic surfactant and an anionic                                             surfactant, manufactured by Toho Chemical                                      Industry Co., Ltd.)                                                            Carplex (tradename for a coagulation-                                                                     4     parts                                         preventing agent composed of a white carbon,                                   manufactured by Shionogi Pharmaceutical Co., Ltd.)                             ______________________________________                                    

The above ingredients are homogeneously pulverized and mixed to form a wettable powder.

    ______________________________________                                         FORMULATION EXAMPLE d-3: Emulsifiable concentrate                              ______________________________________                                         Compound No. 3-d of the present invention                                                                 5     parts                                         Xylene                     75    parts                                         N,N-dimethylformamide      15    parts                                         Sorpol 2680 (tradename for a mixture of a                                                                 5     parts                                         nonionic surfactant and an anionic                                             surfactant, manufactured by Toho Chemical                                      Industry Co., Ltd.)                                                            ______________________________________                                    

The above ingredients are homogeneously mixed to form an emulsifiable concentrate.

    ______________________________________                                         FORMULATION EXAMPLE d-4: Flowable                                              ______________________________________                                         Compound No. 4-d of the present invention                                                                25     parts                                         Agrizole S-710 (tradename for a nonionic                                                                 10     parts                                         surfactant, manufactured by Kao Corp.)                                         Runox 1000C (tradename for an anionic                                                                    0.5    part                                          surfactant, manufactured by Toho Chemical                                      Industry Co., Ltd.)                                                            1% Rodopol water (tradename for a thickener,                                                             20     parts                                         manufactured by Rhone-Poulenc)                                                 Water                     44.5   parts                                         ______________________________________                                    

The above ingredients were homogeneously mixed to obtain a flowable.

    ______________________________________                                         FORMULATION EXAMPLE d-5: Flowable                                              ______________________________________                                         Compound No. 5-d of the present invention                                                                40     parts                                         Agrizole S-710 (tradename for a nonionic                                                                 10     parts                                         surfactant, manufactured by Kao Corp.)                                         Runox 1000C (tradename for an anionic                                                                    0.5    part                                          surfactant, manufactured by Toho Chemical                                      Industry Co., Ltd.)                                                            1% Rodopol water (tradename for a thickener,                                                             20     parts                                         manufactured by Rhone-Poulenc)                                                 Water                     29.5   parts                                         ______________________________________                                    

The above ingredients were homogeneously mixed to obtain a flowable.

    ______________________________________                                         FORMULATION EXAMPLE d-6: Granular wettable powder                              (dry flowable)                                                                 ______________________________________                                         Compound No. 6-d of the present invention                                                                 75    parts                                         Isoban No. 1 (tradename for an anionic                                                                    10    parts                                         surfactant, manufactured by Kuraray Isoprene                                   Chemical Co., Ltd.)                                                            Vanirex N (tradename for an anionic                                                                       5     parts                                         surfactant, manufactured by Sanyo Kokusaku                                     Pulp Co., Ltd.)                                                                Carplex #80 (tradename for a white carbon,                                                                10    parts                                         manufactured by Shionogi Pharmaceutical Co., Ltd.)                             ______________________________________                                    

The above ingredients are uniformly mixed and pulverized to form a dry flowable.

    ______________________________________                                         FORMULATION EXAMPLE d-7: Granule                                               ______________________________________                                         Compound No. 9-d of the present invention                                                                 1     part                                          Bentonite                  55    parts                                         Talc                       44    parts                                         ______________________________________                                    

The above ingredients were homogeneously mixed and pulverized, and after an addition of a small amount of water, the mixture was stirred, mixed and granulated by an extrusion-type granulating machine, followed by drying to obtain a granule.

    ______________________________________                                         FORMULATION EXAMPLE e-1: Wettable powder                                       ______________________________________                                         Compound No. 1-e of the present invention                                                                 20    parts                                         Zeeklite A (tradename for a kaolin-type                                                                   76    parts                                         clay, manufactured by Zeeklite Industries, Co., Ltd.)                          Sorpol 5039 (tradename for a mixture of a                                                                 2     parts                                         nonionic surfactant and an anionic                                             surfactant, manufactured by Toho Chemical                                      Industry Co., Ltd.)                                                            Carplex (tradename for a coagulation-                                                                     2     parts                                         preventing agent composed of a white carbon,                                   manufactured by Shionogi Pharmaceutical Co., Ltd.)                             ______________________________________                                    

The above ingredients are homogeneously pulverized and mixed to form a wettable powder.

    ______________________________________                                         FORMULATION EXAMPLE e-2: Wettable powder                                       ______________________________________                                         Compound No. 2-e of the present invention                                                                 40    parts                                         Zeeklite A (tradename for a kaolin-type                                                                   54    parts                                         clay, manufactured by Zeeklite Industries, Co., Ltd.)                          Sorpol 5039 (tradename for a mixture of a                                                                 2     parts                                         nonionic surfactant and an anionic                                             surfactant, manufactured by Toho Chemical                                      Industry Co., Ltd.)                                                            Carplex (tradename for a coagulation-                                                                     4     parts                                         preventing agent composed of a white carbon,                                   manufactured by Shionogi Pharmaceutical Co., Ltd.)                             ______________________________________                                    

The above ingredients are homogeneously pulverized and mixed to form a wettable powder.

    ______________________________________                                         FORMULATION EXAMPLE e-3: Emulsifiable concentrate                              ______________________________________                                         Compound No. 3-e of the present invention                                                                 5     parts                                         Xylene                     75    parts                                         N,N-dimethylformamide      15    parts                                         Sorpol 2680 (tradename for a mixture of a                                                                 5     parts                                         nonionic surfactant and an anionic                                             surfactant, manufactured by Toho Chemical                                      Industry Co., Ltd.)                                                            ______________________________________                                    

The above ingredients are homogeneously mixed to form an emulsifiable concentrate.

    ______________________________________                                         FORMULATION EXAMPLE e-4: Flowable                                              ______________________________________                                         Compound No. 4-e of the present invention                                                                25     parts                                         Agrizole S-710 (tradename for a nonionic                                                                 10     parts                                         surfactant, manufactured by Kao Corp.)                                         Runox 1000C (tradename for an anionic                                                                    0.5    part                                          surfactant, manufactured by Toho Chemical                                      Industry Co., Ltd.)                                                            1% Rodopol water (tradename for a thickener,                                                             20     parts                                         manufactured by Rhone-Poulenc)                                                 Water                     44.5   parts                                         ______________________________________                                    

The above ingredients were homogeneously mixed to obtain a flowable.

    ______________________________________                                         FORMULATION EXAMPLE e-5: Flowable                                              ______________________________________                                         Compound No. 5-e of the present invention                                                                40     parts                                         Agrizole S-710 (tradename for a nonionic                                                                 10     parts                                         surfactant, manufactured by Kao Corp.)                                         Runox 1000C (tradename for an anionic                                                                    0.5    parts                                         surfactant, manufactured by Toho Chemical                                      Industry Co., Ltd.)                                                            1% Rodopol water (tradename for a thickener,                                                             20     parts                                         manufactured by Rhone-Poulenc)                                                 Water                     29.5   parts                                         ______________________________________                                    

The above ingredients were homogeneously mixed to obtain a flowable.

    ______________________________________                                         FORMULATION EXAMPLE e-6: Granular wettable powder                              (dry flowable)                                                                 ______________________________________                                         Compound No. 1-e of the present invention                                                                 75    parts                                         Isoban No. 1 (tradename for an anionic                                                                    10    parts                                         surfactant, manufactured by Kuraray Isoprene                                   Chemical Co., Ltd.)                                                            Vanirex N (tradename for an anionic                                                                       5     parts                                         surfactant, manufactured by Sanyo Kokusaku                                     Pulp Co., Ltd.)                                                                Carplex #80 (tradename for a white carbon,                                                                10    parts                                         manufactured by Shionogi Pharmaceutical Co., Ltd.)                             ______________________________________                                    

The above ingredients are uniformly mixed and pulverized to form a dry flowable.

    ______________________________________                                         FORMULATION EXAMPLE e-7: Granule                                               ______________________________________                                         Compound No. 5-e of the present invention                                                                1     part                                           Bentonite                 55    parts                                          Talc                      44    parts                                          ______________________________________                                    

The above ingredients were homogeneously mixed and pulverized, and after an addition of a small amount of water, the mixture was stirred, mixed and granulated by an extrusion-type granulating machine, followed by drying to obtain a granule.

    ______________________________________                                         FORMULATION EXAMPLE f-1: Wettable powder                                       ______________________________________                                         Compound No. 1-f of the present invention                                                                  20 parts                                           Zeeklite A (tradename for a kaolin-type                                                                    76 parts                                           clay, manufactured by Zeeklite Industries,                                     Co., Ltd.)                                                                     Sorpol 5039 (tradename for a mixture of a                                                                   2 parts                                           nonionic surfactant and an anionic                                             surfactant, manufactured by Toho Chemical                                      Industry Co., Ltd.)                                                            Carplex (tradename for a coagulation-                                                                       2 parts                                           preventing agent composed of a white carbon,                                   manufactured by Shionogi Pharmaceutical                                        Co., Ltd.)                                                                     ______________________________________                                    

The above ingredients are homogeneously pulverized and mixed to form a wettable powder.

    ______________________________________                                         FORMULATION EXAMPLE f-2: Wettable powder                                       ______________________________________                                         Compound No. 2-f of the present invention                                                                  40 parts                                           Zeeklite A (tradename for a kaolin-type                                                                    54 parts                                           clay, manufactured by Zeeklite Industries,                                     Co., Ltd.)                                                                     Sorpol 5039 (tradename for a mixture of a                                                                   2 parts                                           nonionic surfactant and an anionic                                             surfactant, manufactured by Toho Chemical                                      Industry Co., Ltd.)                                                            Carplex (tradename for a coagulation-                                                                       4 parts                                           preventing agent composed of a white carbon,                                   manufactured by Shionogi Pharmaceutical                                        Co., Ltd.)                                                                     ______________________________________                                    

The above ingredients are homogeneously pulverized and mixed to form a wettable powder.

    ______________________________________                                         FORMULATION EXAMPLE f-3: Emulsifiable                                          concentrate                                                                    ______________________________________                                         Compound No. 1-f of the present invention                                                                   5 parts                                           Xylene                      75 parts                                           N,N-dimethylformamide       15 parts                                           Sorpol 2680 (tradename for a mixture of a                                                                   5 parts                                           nonionic surfactant and an anionic                                             surfactant, manufactured by Toho Chemical                                      Industry Co., Ltd.)                                                            ______________________________________                                    

The above ingredients are homogeneously mixed to form an emulsifiable concentrate.

    ______________________________________                                         FORMULATION EXAMPLE f-4: Flowable                                              ______________________________________                                         Compound No. 2-f of the present invention                                                                25     parts                                         Agrizole S-710 (tradename for a nonionic                                                                 10     parts                                         surfactant, manufactured by Kao Corp.)                                         Runox 1000C (tradename for an anionic                                                                    0.5    part                                          surfactant, manufactured by Toho Chemical                                      Industry Co., Ltd.)                                                            1% Rodopol water (tradename for a thickener,                                                             20     parts                                         manufactured by Rhone-Poulenc)                                                 Water                     44.5   parts                                         ______________________________________                                    

The above ingredients were homogeneously mixed to obtain a flowable.

    ______________________________________                                         FORMULATION EXAMPLE f-5: Flowable                                              ______________________________________                                         Compound No. 2-f of the present invention                                                                40     parts                                         Agrizole S-710 (tradename for a nonionic                                                                 10     parts                                         surfactant, manufactured by Kao Corp.)                                         Runox 1000C (tradename for an anionic                                                                    0.5    part                                          surfactant, manufacture, by Toho Chemical                                      Industry Co., Ltd.)                                                            1% Rodopol water (tradename for a thickener,                                                             20     parts                                         manufactured by Rhone-Poulenc)                                                 Water                     29.5   parts                                         ______________________________________                                    

The above ingredients were homogeneously mixed to obtain a flowable.

    ______________________________________                                         FORMULATION EXAMPLE f-6: Granular wettable powder                              (dry flowable)                                                                 ______________________________________                                         Compound No. 2-f of the present invention                                                                 75    parts                                         Isoban No. 1 (tradename for an anionic                                                                    10    parts                                         surfactant, manufactured by Kuraray Isoprene                                   Chemical Co., Ltd.)                                                            Vanirex N (tradename for an anionic                                                                       5     parts                                         surfactant, manufactured by Sanyo Kokusaku                                     Pulp Co., Ltd.)                                                                Carplex #80 (tradename for a white carbon,                                                                10    parts                                         manufactured by Shionogi Pharmaceutical Co., Ltd.)                             ______________________________________                                    

The above ingredients are uniformly mixed and pulverized to form a dry flowable.

    ______________________________________                                         FORMULATION EXAMPLE f-7: Granule                                               ______________________________________                                         Compound No. 2-f of the present invention                                                                 1     part                                          Bentonite                  55    parts                                         Talc                       44    parts                                         ______________________________________                                    

The above ingredients were homogeneously mixed and pulverized, and after an addition of a small amount of water, the mixture was stirred, mixed and granulated by an extrusion-type granulating machine, followed by drying to obtain a granule.

    ______________________________________                                         FORMULATION EXAMPLE g-1: Wettable powder                                       ______________________________________                                         Compound No. 1-g of the present invention                                                                  20 parts                                           Zeeklite A (tradename for a kaolin-type                                                                    76 parts                                           clay, manufactured by Zeeklite Industries,                                     Co., Ltd.)                                                                     Sorpol 5039 (tradename for a mixture of a                                                                   2 parts                                           nonionic surfactant and an anionic                                             surfactant, manufactured by Toho Chemical                                      Industry Co., Ltd.)                                                            Carplex (tradename for a coagulation-                                                                       2 parts                                           preventing agent composed of a white carbon,                                   manufactured by Shionogi Pharmaceutical                                        Co., Ltd.)                                                                     ______________________________________                                    

The above ingredients are homogeneously pulverized and mixed to form a wettable powder.

    ______________________________________                                         FORMULATION EXAMPLE g-2: Wettable powder                                       ______________________________________                                         Compound No. 2-g of the present invention                                                                  40 parts                                           Zeeklite A (tradename for a kaolin-type                                                                    54 parts                                           clay, manufactured by Zeeklite Industries,                                     Co., Ltd.)                                                                     Sorpol 5039 (tradename for a mixture of a                                                                   2 parts                                           nonionic surfactant and an anionic                                             surfactant, manufactured by Toho Chemical                                      Industry Co., Ltd.)                                                            Carplex (tradename for a coagulation-                                                                       4 parts                                           preventing agent composed of a white carbon,                                   manufactured by Shionogi Pharmaceutical                                        Co., Ltd.)                                                                     ______________________________________                                    

The above ingredients are homogeneously pulverized and mixed to form a wettable powder.

    ______________________________________                                         FORMULATION EXAMPLE g-3: Emulsifiable                                          concentrate                                                                    ______________________________________                                         Compound No. 3-g of the present                                                                      5 parts                                                  invention                                                                      Xylene               75 parts                                                  N,N-dimethylformamide                                                                               15 parts                                                  Sorpol 2680 (tradename for a mixture of                                                              5 parts                                                  a nonionic surfactant and an anionic                                           surfactant, manufactured by Toho                                               Chemical Industry Co., Ltd.)                                                   ______________________________________                                    

The above ingredients are homogeneously mixed to form an emulsifiable concentrate.

    ______________________________________                                         FORMULATION EXAMPLE g-4: Flowable                                              ______________________________________                                         Compound No. 4-g of the present invention                                                                25     parts                                         Agrizole S-710 (tradename for a nonionic                                                                 10     parts                                         surfactant, manufactured by Kao Corp.)                                         Runox 1000C (tradename for an anionic                                                                    0.5    part                                          surfactant, manufactured by Toho Chemical                                      Industry Co., Ltd.)                                                            1% Rodopol water (tradename for a thickener,                                                             20     parts                                         manufactured by Rhone-Poulenc)                                                 Water                     44.5   parts                                         ______________________________________                                    

The above ingredients were homogeneously mixed to obtain a flowable.

    ______________________________________                                         FORMULATION EXAMPLE g-5: Flowable                                              ______________________________________                                         Compound No. 5-g of the present invention                                                                40     parts                                         Agrizole S-710 (tradename for a nonionic                                                                 10     parts                                         surfactant, manufactured by Kao Corp.)                                         Runox 1000C (tradename for an anionic                                                                    0.5    part                                          surfactant, manufactured by Toho Chemical                                      Industry Co., Ltd.)                                                            1% Rodopol water (tradename for a thickener,                                                             20     parts                                         manufactured by Rhone-Poulenc)                                                 Water                     29.5   parts                                         ______________________________________                                    

The above ingredients were homogeneously mixed to obtain a flowable.

    ______________________________________                                         FORMULATION EXAMPLE g-6: Granular wettable                                     powder (dry flowable)                                                          ______________________________________                                         Compound No. 12-g of the present invention                                                                 75 parts                                           Isoban No. 1 (tradename for an anionic                                                                     10 parts                                           surfactant, manufactured by Kuraray Isoprene                                   Chemical Co., Ltd.)                                                            Vanirex N (tradename for an anionic                                                                         5 parts                                           surfactant, manufactured by Sanyo Kokusaku                                     Pulp Co., Ltd.)                                                                Carplex #80 (tradename for a white carbon,                                                                 10 parts                                           manufactured by Shionogi Pharmaceutical                                        Co., Ltd.)                                                                     ______________________________________                                    

The above ingredients are uniformly mixed and pulverized to form a dry flowable.

    ______________________________________                                         FORMULATION EXAMPLE g-7: Granule                                               ______________________________________                                         Compound No. 19-g of the present invention                                                               1     part                                           Bentonite                 55    parts                                          Talc                      44    parts                                          ______________________________________                                    

The above ingredients were homogeneously mixed and pulverized, and after an addition of a small amount of water, the mixture was stirred, mixed and granulated by an extrusion-type granulating machine, followed by drying to obtain a granule.

In use, the above wettable powder, emulsifiable concentrate, flowable or granular wettable powder is diluted with water from 50 to 1,000 times and applied so that the active ingredient will be from 0.0001 to 10 kg per hectare (ha).

Now, the herbicidal activities of the compounds of the present invention will be described in detail with reference to the following Test Examples.

TEST EXAMPLE 1: Test-1 on the Herbicidal Effects in Soil Treatment

A plastic box having a length of 15 cm, a width of 22 cm and a depth of 6 cm was filled with a sterilized diluvial soil, and seeds of Echinochloa crus-galli, Digitaria adscendens, Cyperus microiria, Solanum nigrum, Galinsoga ciliata, Rorippa indica, Oryza sativa, Zea mays, Triticum aestivum, Glycine max and Gossypium spp. were sown, and the soil was covered thereon in a thickness of about 1.5 cm, and then a herbicide solution was applied onto the surface of the soil uniformly so that the active ingredient was distributed at a predetermined concentration. The herbicide solution was prepared by diluting a wettable powder prepared in accordance with the foregoing Formulation Examples with water and applied by a small spray onto the entire soil surface. Four weeks after the application of the herbicidal solution, the herbicidal effects against each weed and the phytotoxicities against each crop plant were determined on the basis of the following standard ratings. The results are shown in Table 15.

Standard ratings:

5: Growth control rate of more than 90% (almost completely withered)

4: Growth control rate of from 70 to 90%

3: Growth control rate of from 40 to 70%

2: Growth control rate of from 20 to 40%

1: Growth control rate of from 5 to 20%

0: Growth control rate of less than 5% (almost non-effective)

The above growth control rates were calculated by the following equation: ##EQU1## where T: Weight of the weed grown above the soil surface of the treated area

N: Weight of the weed grown above the soil surface of the non-treated area

TEST EXAMPLE 2: Test-1 on the Herbicidal Effects in Foliage Treatment

A plastic box having a length of 15 cm, a width of 22 cm and a depth of 6 cm was filled with a sterilized diluvial soil, and seeds of Echinochloa crus-galli, Digitaria adscendens, Avena fatua, Cyperus microiria, Solanum nigrum, Galinsoga ciliata, Rorippa indica, Oryza sativa, Zea mays, Triticum aestivum, Glycine max, Gossypium spp. and Beta vulgaris were spot-wisely sown, and the soil was covered thereon in a thickness of about 1.5 cm. When the various weeds and crop plants grew to the 2 or 3 leaf stage, a herbicidal solution was uniformly sprayed on the foliages so that the active ingredient was applied in a predetermined concentration. The herbicidal solution was prepared by diluting a wettable powder prepared in accordance with the above Formulation Examples with water and applied onto the entire surface of the foliages of the weeds and the crop plants by a small spray. Four weeks after the application of the herbicide solution, the herbicidal effects against each weed and the phytotoxicities against each crop plant were determined on the basis of the standard ratings described in Test Example 1. The results are shown in Table 16.

TEST EXAMPLE 3: Test-1 on the Herbicidal Effects in Irrigation Treatment

Into a Wagner pot of 1/5000a, alluvial soil was put, and then water was introduced and mixed to form an irrigated state with a water depth of 4 cm. Seeds of Echinochloa crus-galli, Scirpus juncoides, Monochoria vaginalis and Rotala indica were sown in the above pot, and tubers of Sagittaria pygmaea and Cyperus serotinus were embedded. Then, rice seedlings of 2.5 leaf stage were transplanted. The pot was placed in a greenhouse at a temperature of from 25° to 30° C., and the plants were cultured. On the third day after the seeding and plantation, a diluted solution of the herbicide was dropwise applied to the water surface by a measuring pipette, so that the dose would be a predetermined level. Three weeks after the dropwise application of the herbicide, the herbicidal effects against various weeds and rice were determined on the basis of the standard ratings described in Test Example 1. The results are shown in Table 17.

In tables 15, 16 and 17, Compound Nos. correspond to Compound Nos. in the Examples, and symbols have the following meanings.

A: Echinochloa crus-galli (barnyardgrass)

B: Digitaria adscendens (large crabgrass)

C: Avena fatua (wild oat)

D: Cyperus microiris (annual sedge)

E: Solanum nigrum (black nightshade)

F: Galinsoga ciliata (hairy galinsoga)

G: Rorippa indica (fieldcress)

H: Scirpus juncoides (bulrush)

I: Monochoria vaginalis (ducksalad)

J: Rotala indica (toothcup)

K: Sagittaria pygmaea (arrowhead)

L: Cyperus serotinus (flat sedge)

a: Oryza sativa (rice)

b: Zea mays (corn)

c: Triticum aestivum (wheat)

d: Glycine max (soybean)

e: Gossypium spp. (cotton)

f: Beta vulgaris (sugar beet)

                  TABLE 15                                                         ______________________________________                                               Dose                                                                                                  No. (kg/ha) A B D E F G a b c d e                 ______________________________________                                          1-a  2.5      4     4   5   1   3   5   5   5   5   4                                                      3                                                                               2-a 0.04 5 5 5 1 5 5 1 0 0 0 0                                                 0.08 5 5 5 1 5 5 2 1 1 0 0                                                     0.16 5 5 5 2 5 5 3 3 2 1 0                                                     3-a 2.5 4 4 1 1 0 4 3 0 2 1 0                                                  6-a 0.63 5 5 5 0 4 4 4 1 3 0 0                                                 7-a 0.04 4 5 5 0 3 4 0 0 0 0 0                                                 0.08 5 5 5 0 4 5 0 0 0 0 0                                                     0.16 5 5 5 2 5 5 2 0 0 0 0                                                     8-a 0.63 5 5 5 2 5 5 3 0 0 0 0                                                10-a 0.16 4 5 5 0 2 4 0 0 0 0 0                                                 0.32 5 5 5 0 4 5 1 0 0 0 0                                                     0.63 5 5 5 0 5 5 3 0 0 0 0                                                    12-a 0.04 5 4 4 0 3 5 0 0 0 0 0                                                 0.08 5 5 5 0 4 5 1 0 0 0 0                                                     0.16 5 5 5 1 5 5 3 1 0 0 0                                                    20-a 0.04 4 2 5 0 3 3 1 0 0 0 0                                                 0.08 5 3 5 0 4 4 2 0 0 0 0                                                     0.16 5 4 5 1 5 5 3 1 0 0 0                                                    22-a 0.16 5 2 5 0 5 5 0 0 0 0 0                                                 0.32 5 3 5 1 5 5 0 0 0 0 0                                                     0.63 5 4 5 1 5 5 1 0 0 0 0                                                    24-a 0.16 5 5 4 0 3 4 0 0 0 0 0                                                 0.32 5 5 5 0 4 5 2 0 0 0 0                                                     0.63 5 5 5 0 5 5 3 1 1 0 0                                                    25-a 0.63 5 5 5 2 4 5 3 1 1 0 0                                                26-a 0.63 4 3 4 0 4 5 0 0 0 0 0                                                30-a 2.5 3 2 5 4 5 5 4 3 2 1 0                                                 31-a 2.5 2 2 5 4 4 5 2 0 1 0 0                                                 34-a 2.5 5 5 5 4 5 5 3 3 5 0 0                                                 36-a 2.5 5 4 5 5 5 5 1 0 0 0 0                                                 38-a 0.63 5 5 5 2 4 5 2 1 0 0 0                                                39-a 2.5 5 5 5 4 4 5 3 1 0 0 0                                                 40-a 0.63 5 5 5 3 4 5 2 1 1 0 0                                                41-a 2.5 5 5 5 4 5 5 4 4 1 1 0                                                 43-a 2.5 3 4 5 3 3 5 0 0 0 0 0                                                 45-a 0.63 5 5 5 0 5 5 0 0 0 0 0                                                47-a 0.63 5 4 5 3 5 5 3 3 1 0 0                                                48-a 0.63 5 4 5 1 5 5 5 3 2 0 0                                                49-a 2.5 5 5 5 2 5 5 3 2 1 0 0                                                 52-a 2.5 5 5 5 3 3 5 4 1 1 0 0                                                 53-a 2.5 5 5 5 3 3 5 5 0 0 0 0                                                 56-a 2.5 5 5 5 3 5 5 4 3 3 3 0                                                 59-a 0.63 5 4 5 5 5 5 1 0 0 0 0                                                61-a 2.5 5 5 5 4 5 5 1 2 1 0 0                                                 63-a 0.63 5 5 5 3 5 5 3 1 2 0 0                                                64-a 2.5 5 5 5 2 5 5 3 2 3 1 0                                                 73-a 0.63 5 5 5 3 5 5 5 5 5 3 0                                                74-a 0.63 5 5 5 2 5 5 3 2 2 0 0                                                 1-b 5 -- -- 4 -- 3 5 -- 0 0 0 --                                               3-b 5 -- -- 3 -- 2 4 -- 0 0 0 --                                               1-c 0.16 5 5 5 2 4 5 5 4 1 4 0                                                 2-c 0.16 5 5 5 4 5 5 5 4 2 0 0                                                 3-c 0.16 5 5 5 2 5 5 5 3 3 1 0                                                 4-c 0.63 4 5 5 2 4 5 1 1 0 0 0                                                 5-c 0.63 5 5 5 1 5 5 1 1 0 0 0                                                 6-c 0.63 2 3 5 0 4 5 1 0 0 0 0                                                 7-c 0.63 5 5 5 2 5 5 4 1 0 1 0                                                 8-c 10 2 4 5 5 4 5 1 0 0 0 0                                                  11-c 0.63 5 5 5 2 5 5 3 2 1 0 0                                                12-c 0.16 5 5 5 2 5 5 4 3 0 0 0                                                13-c 0.16 5 5 5 4 5 5 4 3 3 0 0                                                14-c 0.63 5 5 5 0 5 5 2 0 0 0 0                                                15-c 0.63 5 5 5 3 5 5 2 1 0 0 0                                                16-c 0.63 5 5 5 4 5 5 4 4 3 0 0                                                17-c 0.63 5 5 5 3 5 5 2 0 0 0 0                                                18-c 0.16 5 5 5 3 5 5 5 2 0 0 0                                                20-c 0.63 0 0 3 3 5 5 0 0 0 0 0                                                23-c 0.63 4 3 5 5 5 5 5 1 2 0 0                                                24-c 0.16 5 5 1 2 5 5 4 1 1 0 0                                                26-c 0.63 5 5 4 2 5 5 5 3 5 3 0                                                35-c 0.16 5 5 5 3 5 5 5 5 4 0 0                                                36-c 0.16 5 5 5 3 5 5 5 4 4 0 0                                                37-c 0.16 5 5 5 4 5 5 5 5 5 4 1                                                38-c 0.63 5 5 5 3 5 5 5 5 2 0 1                                                39-c 0.63 5 5 5 3 5 5 4 4 3 1 0                                                40-c 0.16 5 5 5 4 5 5 5 5 5 2 2                                                 2-d 2.5 4 5 5 5 4 5 0 0 0 0 0                                                  3-d 2.5 5 5 5 5 0 5 0 0 0 0 0                                                  5-d 2.5 3 5 5 5 3 5 3 0 0 0 0                                                  6-d 10 2 4 5 5 5 5 1 0 0 0 1                                                   9-d 10 3 5 5 5 5 5 3 1 1 0 0                                                   1-e 5 5 5 5 2 2 5 5 1 0 0 0                                                    2-e 2.5 3 3 2 1 0 2 0 0 0 0 0                                                  4-e 5 3 5 5 3 3 5 1 0 0 0 0                                                    2-f 10 4 5 5 5 5 5 4 0 1 0 0                                                   1-g 0.63 5 5 5 5 5 5 3 0 1 1 0                                                 7-g 2.5 5 5 5 3 5 5 3 1 4 2 1                                                  9-g 2.5 5 5 5 5 5 5 0 0 0 0 0                                                 11-g 0.63 5 5 5 3 5 5 3 2 1 1 0                                                12-g 2.5 5 4 5 3 5 5 1 1 1 0 0                                                 13-g 2.5 5 3 5 3 5 5 1 0 1 0 0                                                 14-g 2.5 4 4 5 3 5 5 0 0 0 0 0                                                 15-g 2.5 5 4 5 3 5 5 1 1 2 0 0                                                 16-g 2.5 5 4 5 3 5 5 3 3 4 0 0                                                 17-g 0.63 5 5 5 5 5 5 3 1 3 0 0                                                18-g 0.63 5 5 5 5 5 5 4 2 2 0 0                                                19-g 2.5 4 5 5 2 5 5 4 3 3 1 0                    ______________________________________                                    

                                      TABLE 16                                     __________________________________________________________________________        Dose                                                                        No.                                                                               (kg/ha)                                                                             A B C D E F G a  b c  d e  f                                           __________________________________________________________________________      1-a                                                                              2.5  4 2 4 2 5 4 4 3  3 3  3 1  3                                            2-a                                                                              0.16 5 2 4 3 4 4 4 2  3 2  3 0  1                                              0.32 5 3 5 4 5 5 5 2  4 2  3 1  2                                              0.63 5 3 5 4 5 5 5 3  4 3  4 2  2                                            3-a                                                                              2.5  4 3 4 2 3 1 2 1  1 2  3 1  1                                            6-a                                                                              2.5  5 3 5 2 3 3 4 4  4 3  3 1  0                                            7-a                                                                              0.16 5 1 3 2 3 2 3 1  3 0  0 1  0                                              0.32 5 2 3 3 5 3 4 2  3 1  1 1  0                                              0.63 5 3 4 3 5 4 5 3  4 3  3 2  2                                            8-a                                                                              2.5  5 1 5 2 5 4 4 3  4 2  4 2  2                                           10-a                                                                              2.5  5 2 5 3 5 3 4 3  3 3  4 1  3                                           12-a                                                                              0.16 4 3 4 3 2 4 4 1  3 0  0 0  0                                              0.32 5 4 5 4 3 5 5 2  3 0  1 0  1                                              0.63 5 5 5 5 4 5 5 3  4 1  2 1  1                                           20-a                                                                              0.16 5 0 2 4 4 4 4 2  4 0  0 0  1                                              0.32 5 1 2 5 5 5 5 3  5 1  1 0  1                                              0.63 5 2 3 5 5 5 5 4  5 2  2 1  1                                           22-a                                                                              0.63 5 1 2 5 5 5 5 2  4 1  2 0  3                                           24-a                                                                              0.63 5 2 4 4 4 5 5 3  4 1  1 0  1                                           30-a                                                                              2.5  3 0 5 4 4 2 5 3  5 1  3 1  3                                           31-a                                                                              2.5  2 0 5 3 4 5 5 3  4 1  1 0  1                                           34-a                                                                              2.5  5 5 3 5 5 4 4 2  5 1  1 0  3                                           36-a                                                                              2.5  4 0 2 4 4 4 3 0  3 0  0 0  0                                           38-a                                                                              2.5  5 3 4 5 5 9 4 4  5 2  3 0  1                                           40-a                                                                              2.5  5 3 5 5 4 3 4 4  5 3  3 1  0                                           47-a                                                                              2.5  5 2 5 5 3 5 5 4  5 1  3 1  3                                           48-a                                                                              2.5  5 2 5 5 5 5 5 5  5 3  4 1  5                                           56-a                                                                              2.5  5 3 5 3 5 3 5 3  4 1  3 0  3                                           59-a                                                                              2.5  5 2 5 5 5 5 5 4  5 2  3 1  5                                           63-a                                                                              2.5  5 3 3 5 5 5 5 3  5 1  4 1  4                                           64-a                                                                              2.5  5 3 5 5 5 5 5 4  5 3  3 0  4                                           73-a                                                                              0.16 5 5 5 4 2 5 5 4  5 4  4 1  0                                           74-a                                                                              0.63 5 5 3 4 5 5 5 1  5 2  1 1  4                                            1-c                                                                              0.16 5 5 5 5 5 5 5 4  5 1  4 1  5                                            2-c                                                                              0.16 5 5 5 5 4 5 5 4  4 2  3 1  4                                            3-c                                                                              0.16 5 5 5 5 5 5 5 5  4 2  4 1  5                                            4-c                                                                              0.63 5 2 1 3 3 5 5 3  4 0  0 0  4                                            5-c                                                                              0.63 5 5 5 5 5 5 5 3  5 3  3 3  5                                            6-c                                                                              0.63 5 5 4 5 5 5 5 2  5 2  4 2  5                                            7-c                                                                              0.63 5 5 4 5 5 5 5 3  4 1  3 3  4                                            8-c                                                                              10   2 2 2 3 5 5 5 0  3 0  0 2  4                                           11-c                                                                              0.63 5 5 5 5 5 5 5 3  4 3  3 4  5                                           12-c                                                                              0.16 5 5 4 5 5 5 5 2  5 1  4 3  5                                           13-c                                                                              0.16 5 5 5 5 5 5 5 3  5 3  5 4  5                                           14-c                                                                              0.63 5 5 5 5 2 5 5 2  4 0  0 3  5                                           15-c                                                                              0.63 5 5 4 5 5 5 5 3  5 0  0 2  5                                           16-c                                                                              0.63 5 5 4 5 5 5 5 3  5 3  4 4  5                                           17-c                                                                              0.63 5 4 3 5 5 5 5 1  5 1  3 3  4                                           18-c                                                                              0.16 5 5 4 5 5 5 5 2  5 3  4 4  5                                           20-c                                                                              0.63 1 1 0 0 5 5 5 0  0 0  0 1  2                                           21-c                                                                              0.63 3 5 2 3 5 5 5 1  3 0  0 1  2                                           23-c                                                                              0.63 5 4 3 5 5 5 5 1  1 0  0 1  1                                           24-c                                                                              0.16 5 5 5 2 3 5 5 4  5 1  5 3  3                                           26-c                                                                              0.63 5 5 5 3 4 5 5 5  5 5  5 0  3                                           35-c                                                                              0.16 5 5 5 5 5 5 5 4  5 4  3 3  5                                           36-c                                                                              0.16 5 5 5 5 5 5 5 4  5 4  4 3  5                                           37-c                                                                              0.16 5 5 5 5 5 5 5 5  5 5  5 3  5                                           38-c                                                                              0.63 5 5 3 5 5 5 5 3  5 2  4 2  5                                           39-c                                                                              0.63 5 5 5 5 4 5 5 4  5 2  5 4  4                                           40-c                                                                              0.16 5 5 5 5 5 5 5 5  5 5  5 4  5                                            5-d                                                                              10   4 5 2 5 5 5 5 2  4 1  3 3  5                                            6-d                                                                              10   3 4 4 5 5 5 5 2  3 1  2 3  5                                            9-d                                                                              10   2 4 4 4 5 5 5 0  4 0  3 2  3                                            1-e                                                                              5    4 2 2 3 5 5 5 3  5 1  2 0  3                                            2-e                                                                              2.5  3 0 0 1 3 0 1 1  0 0  0 0  1                                            4-e                                                                              5    2 0 4 4 5 5 3 2  3 0  0 0  4                                            2-f                                                                              10   3 0 2 2 5 5 4 1  3 0  2 0  3                                            1-g                                                                              2.5  5 4 --                                                                               5 5 5 5 4  4 2  4 1  4                                            7-g                                                                              2.5  2 3 5 5 5 5 5 1  5 2  4 3  5                                            9-g                                                                              2.5  2 3 4 5 5 4 5 0  3 1  5 2  5                                           11-g                                                                              2.5  5 5 3 5 5 5 5 2  5 4  4 3  4                                           12-g                                                                              2.5  4 3 3 3 5 5 5 0  4 1  4 1  3                                           13-g                                                                              2.5  4 2 3 3 5 5 5 0  4 1  4 1  3                                           14-g                                                                              2.5  3 1 3 3 5 5 5 0  4 1  4 1  3                                           15-g                                                                              2.5  4 3 5 5 5 5 5 1  5 3  4 2  4                                           16-g                                                                              2.5  5 3 5 5 5 5 5 2  5 3  5 2  4                                           17-g                                                                              2.5  5 5 5 4 5 5 5 5  5 5  5 1  3                                           18-g                                                                              2.5  5 5 5 4 5 5 5 5  5 5  5 3  5                                           19-g                                                                              2.5  3 2 2 3 5 5 3 1  4 2  3 2  3                                           __________________________________________________________________________

                  TABLE 17                                                         ______________________________________                                               Dose                                                                     No.   (kg/ha)   A      H    I    J    K    L    a                              ______________________________________                                         74-a  2.5       5      4    4    4    5    4    0                               1-b  4         4      --   5    5    5    --   0                               1-c  0.64      5      5    4    5    5    5    0                               7-c  2.5       5      0    4    4    4    4    0                              13-c  0.64      5      4    5    4    5    5    0                              50-c  0.64      5      4    5    5    5    4    0                              53-c  0.16      5      0    4    5    4    2    0                              54-c  0.16      5      2    4    4    5    5    0                              ______________________________________                                    

TEST EXAMPLE 4: Test-2 on the Herbicidal Effects in Soil Treatment

A plastic box having a length of 21 cm, a width of 13 cm and a depth of 7 cm was filled with a sterilized diluvial soil, and seeds of Echinochloa crus-galli, Setaria viridis, Avena fatua, Alopecurus myosuroides, Abutilon theophrasti, Xanthium strumarium, Amaranthus viridis, Ipomoea spp., Veronica persica, Stellaria media, Zea mays, Oryza sativa, Oryza sativa, Glycine max, Gossypium spp., Triticum aestivum and Beta vulgaris were spot-wisely sown, and the soil was covered thereon in a thickness of about 1.5 cm, and then a herbicide solution was applied onto the surface of the soil uniformly so that the active ingredient was distributed at a predetermined concentration. The herbicide solution was prepared by diluting a wettable powder prepared in accordance with the foregoing Formulation Examples with water and applied onto the entire soil surface by a small spray. Three weeks after the application of the herbicidal solution, the herbicidal effects against each weed and the phytotoxicities against each crop plant were visually determined on the basis of the following standard ratings. The results are shown in Table 18.

Some of the compounds of the present invention show selectivity for certain crop plants.

Standard ratings:

5: Growth control rate of more than 90% (almost completely withered)

4: Growth control rate of from 70 to 90%

3: Growth control rate of from 40 to 70%

2: Growth control rate of from 20 to 40%

1: Growth control rate of from 5 to 20%

0: Growth control rate of less than 5% (almost non-effective)

TEST EXAMPLE 5: Test-2 on the Herbicidal Effects in Foliage Treatment

A plastic box having a length of 21 cm, a width of 13 cm and a depth of 7 cm was filled with a sterilized diluvial soil, and seeds of Echinochloa crus-galli, Setaria viridis, Avena fatua, Alopecurus myosuroides, Abutilon theophrasit, Xanthium strumarium, Amaranthus viridis, Ipomoea spp., Veronica persica, Stellaria media, Zea mays, Oryza sativa, Glycine max, Gossypium spp., Triticum aestivum and Beta vulgaris were spot-wisely sown and the soil was covered thereon in a thickness of about 1.5 cm. When the various weeds and crop plants grew to the 2 or 3 leaf stage, a herbicidal solution was uniformly sprayed on the foliages so that the active ingredient was applied in a predetermined concentration. The herbicidal solution was prepared by diluting a wettable powder prepared in accordance with the above Formulation Examples with water and applied onto the entire surface of the foliages of the weeds and the crop plants by a small spray. Three weeks after the application of the herbicide solution, the herbicidal effects against each weed and the phytotoxicities against each crop plant were visually determined on the basis of the standard ratings described in Test Example 4. The results are shown in Table 19.

TEST EXAMPLE 6:

Test-2 on the Herbicidal Effects During the Growing Stage in Irrigation Treatment

Into a Wagner pot of 1/5000a, alluvial soil was put, and then water was introduced and mixed to form an irrigated state with a water depth of 4 cm. Seeds of Echinochloa crus-galli, Scirpus juncoides, Monochoria vaginalis and Rotala indica were sown in the above pot. The pot was placed in a greenhouse at a temperature of from 25° to 30° C., and the plants were cultured. When Echinochloa crus-galli, Scirpus juncoides, Monochoria vaginalis and Rotala indica reached 1 to 2 leaf stage, a diluted solution of the herbicide was dropwise applied to the water surface by a measuring pipette, so that the dose would be a predetermined level. Three weeks after the dropwise application of the herbicide, the herbicidal effects to various weeds were visually determined on the basis of the standard ratings described in Test Example 4. The results are shown in Table 20.

In Tables 18, 19 and 20, Nos. correspond to Compound Nos. in the Examples, and symbols have the following meanings.

A: Echinochloa crus-galli (barnyardgrass)

B: Setaria viridis (green foxtail)

C: Avena fatua (wild oat)

D: Alopecurus myosuroides (black grass)

E: Abutilon theophrasti (velvetleaf)

F: Xanthium strumarium (common cocklebur)

G: Amaranthus viridis (slender amaranth)

H: Ipomoea spp. (mornigglory)

I: Veronica persica (Persian speedwell)

J: Stellaria media (common chickweed)

a: Zea mays (corn)

b: Oryza sativa (rice)

c: Glycine max (soybean)

d: Gossypium spp. (cotton)

e: Triticum aestivum (wheat)

f: Beta vulgaris (sugar beet)

K: Scirpus juncoides

L: Monochoria vaginalis

M: Rotala indica

                                      TABLE 18                                     __________________________________________________________________________        Dose                                                                        No.                                                                               (kg/ha)                                                                             A B C D E F G H I J a b c d e f                                        __________________________________________________________________________     41-c                                                                              0.16 5 5 3 5 5 5 5 4 2 5 4 5 3 0 3 4                                        43-c                                                                              0.63 5 5 3 5 3 1 5 3 5 5 5 5 1 0 4 4                                        44-c                                                                              0.63 5 5 5 5 5 3 5 5 5 5 5 5 4 0 4 4                                        49-c                                                                              0.63 5 5 2 5 5 2 5 5 5 5 5 5 0 2 2 5                                        50-c                                                                              0.63 5 5 4 5 5 2 5 5 5 5 5 5 1 1 3 5                                        51-c                                                                              0.16 5 5 4 5 5 5 5 5 5 5 5 5 3 1 2 4                                        52-c                                                                              0.63 5 5 5 5 2 5 5 5 5 5 5 5 3 3 4 4                                        53-c                                                                              0.16 5 5 5 5 2 5 5 5 5 5 4 5 0 0 4 5                                        54-c                                                                              0.63 5 5 5 5 5 5 5 5 5 5 5 5 3 1 4 5                                        55-c                                                                              0.63 5 5 5 5 4 5 5 5 5 5 5 5 1 0 5 5                                        56-c                                                                              0.63 5 5 5 5 5 5 5 5 5 5 5 5 3 1 5 5                                        20-g                                                                              0.63 5 5 3 5 5 2 5 3 5 5 4 4 2 0 2 5                                        __________________________________________________________________________

                                      TABLE 19                                     __________________________________________________________________________        Dose                                                                        No.                                                                               (kg/ha)                                                                             A B C D E F G H I J a b c d e f                                        __________________________________________________________________________     41-c                                                                              0.16 5 5 4 5 5 5 5 5 1 5 5 3 4 2 2 5                                        43-c                                                                              0.63 5 5 4 5 5 5 5 3 2 5 5 3 0 1 2 5                                        44-c                                                                              0.63 5 5 5 5 5 5 5 5 3 5 5 4 4 3 3 5                                        49-c                                                                              0.63 5 5 2 5 5 5 5 5 5 5 5 2 4 2 1 5                                        50-c                                                                              0.63 5 5 3 5 5 5 5 5 4 5 5 3 4 3 1 5                                        51-c                                                                              0.16 5 5 3 4 5 5 5 5 5 5 5 4 5 1 2 5                                        52-c                                                                              0.63 5 5 5 5 5 5 5 4 2 5 5 4 4 1 4 5                                        53-c                                                                              0.16 5 5 5 5 5 5 5 5 5 5 5 5 5 3 4 5                                        54-c                                                                              0.16 5 5 5 5 5 5 5 5 5 5 5 5 5 3 3 5                                        55-c                                                                              0.16 5 5 5 5 5 5 5 3 5 5 5 5 5 1 5 5                                        56-c                                                                              0.16 5 5 5 5 5 5 5 2 5 5 5 5 5 1 5 5                                        20-g                                                                              0.63 5 5 5 5 5 5 5 4 5 5 5 5 5 3 4 5                                        __________________________________________________________________________

                  TABLE 20                                                         ______________________________________                                                 Dose                                                                   No.     (kg/ha)      A     K       L   M                                       ______________________________________                                         50-c    0.64         5     4       4   4                                       53-c    0.16         5     3       4   2                                       54-C    0.16         5     4       4   4                                       ______________________________________                                    

INDUSTRIAL APPLICABILITY

Iminosulfonylurea derivatives of the formula (1) of the present invention can be used safely to important crop plants, and they are compounds showing high herbicidal effects against many weeds and thus useful as active ingredients of herbicides. 

We claim:
 1. A compound of the formula: ##STR1199## where Q is ##STR1200## where R^(a1) is CH₂ CH₂ CH₂ F, and Gn is ##STR1201##
 2. A compound of the formula ##STR1202## where Q is ##STR1203## R^(a1) is a C₁₋₈ alkyl group, a C₃₋₇ cycloalkyl group, a C₁₋₆ alkyl group substituted by a C₃₋₇ cycloalkyl group, a C₃₋₇ cycloalkenyl group, a C₁₋₆ alkyl group substituted by a C₃₋₇ cycloalkenyl group, a C₂₋₈ alkenyl group, a C₂₋₈ alkynyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkoxy group, a C₁₋₆ alkyl group substituted by a C₂₋₆ alkenyloxy group, a C₁₋₆ alkyl group substituted by a C₂₋₆ alkynyloxy group, a C₁₋₆ alkyl group substituted by a mono-, di- or poly-halogeno C₁₋₆ alkoxy group, a C₁₋₆ alkyl group substituted by a mono-, di- or polyhalogeno C₂₋₆ alkenyloxy group, a C₁₋₆ alkyl group substituted by a mono-, di- or poly-halogeno C₂₋₆ alkynyloxy group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylthio group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylsulfinyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylsulfonyl group, a mono-, di- or poly-halogeno C₁₋₈ alkyl group, a mono-, di- or poly-halogeno C₂₋₈ alkenyl group, a mono-, di- or poly-halogen C₂₋₈ alkynyl group, a C₁₋₆ alkyl group substituted by a cyano group, a C₂₋₆ alkenyl group substituted by a cyano group, a C₂₋₆ alkynyl group substituted by a cyano group, a C₁₋₆ alkyl group substituted by a nitro group, a C₂₋₆ alkenyl group substituted by a nitro group, a C₂₋₆ alkynyl group substituted by a nitro group, a C₁₋₆ alkyl group substituted by a C₂₋₇ alkoxycarbonyl group, a C₂₋₆ alkenyl group substituted by a C₂₋₇ alkoxycarbonyl group, a C₂₋₆ alkynyl group substituted by a C₂₋₇ alkoxycarbonyl group, a C₁₋₆ alkyl group substituted by a C₂₋₇ alkylcarbonyl group, a C₁₋₆ alkyl group substituted by a mono-, di- or poly-halogeno C₂₋₇ alkylcarbonyl group, a C₁₋₆ alkyl group substituted by a C₃₋₇ alkenylcarbonyl group, a C₁₋₆ alkyl group substituted by a C₃₋₇ alkynylcarbonyl group, a C₁₋₆ alkyl group substituted by a C₂₋₅ alkylcarbonyl group substituted by a C₁₋₄ alkoxy group, a C₁₋₆ alkyl group substituted by a C₂₋₅ alkylcarbonyl group substituted by a C₁₋₄ alkylthio group, a C₁₋₆ alkyl group substituted by a C₂₋₅ alkylcarbonyl group substituted by a C₁₋₄ alkylsulfinyl group, a C₁₋₆ alkyl group substituted by a C₂₋₅ alkylcarbonyl group substituted by a C₁₋₄ alkylsulfonyl group, a C₂₋₆ alkenyl group substituted by a C₂₋₇ alkylcarbonyl group, a C₂₋₆ alkynyl group substituted by a C₂₋₇ alkylcarbonyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylsulfamoyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkoxysulfamoyl group, a C₁₋₆ alkyl group substituted by a di(C₁₋₃ alkyl)sulfamoyl group, a C₁₋₆ alkyl group substituted by an N-(C₁₋₃ alkyl)-N-(C₁₋₃ alkoxy)sulfamoyl group, a C₁₋₆ alkyl group substituted by a C₂₋₇ alkylcarbamoyl group, a C₁₋₆ alkyl group substituted by a di(C₁₋₃ alkyl)carbamoyl group, a C₁₋₆ alkyl group substituted by a C₂₋₇ alkoxycarbamoyl group, a C₁₋₆ alkyl group substituted by an N-(C₁₋₃ alkyl)-N-(C₁₋₄ alkoxy)carbamoyl group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkylamino group, a C₁₋₆ alkyl group substituted by a C₁₋₆ alkoxyamino group, a C₁₋₆ alkyl group substituted by a di(C₁₋₃ alkyl)amino group, a C₁₋₆ alkyl group substituted by an N-(C₁₋₃ alkyl)-N-(C₁₋₃ alkoxy)amino group, a C₁₋₆ alkyl group substituted by an N-(C₂₋₇ alkylcarbonyl)-N-(C₁₋₆ alkyl)amino group, a C₁₋₆ alkyl group substituted by an N-(C₂₋₇ alkylcarbonyl)-N-(C₁₋₆ alkoxy)amino group, a C₁₋₆ alkyl group substituted by an N-(C₁₋₆ alkylsulfonyl)-N-(C₁₋₆ alkyl)amino group, a C₁₋₆ alkyl group substituted by an N-(C₁₋₆ alkylsulfonyl)-N-(C₁₋₆ alkoxy)amino group, a phenyl group (provided that such a phenyl group may be substituted by one or more substitutents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenyl group (provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₂₋₇ alkenyl group substituted by a phenyl group (provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₂₋₆ alkynyl group substituted by a phenyl group (provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenoxy group (provided that such a phenoxy group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenylthio group (provided that such a phenylthio group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenylsulfinyl group (provided that such a phenylsulfinyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenylsulfonyl group (provided that such a phenylsulfonyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a benzyloxy group (provided that the phenyl group of such a benzyloxy group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a benzylthio group (provided that the phenyl group of such a benzylthio group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a benzylsulfinyl group (provided that the phenyl group of such a benzylsulfinyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a benzylsulfonyl group (provided that the phenyl group of such a benzylsulfonyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a phenylcarbonyl group (provided that such a phenylcarbonyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by a benzylcarbonyl group (provided that the phenyl group of such a benzylcarbonyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group), a C₁₋₆ alkyl group substituted by an amino group substituted by a C₁₋₄ alkylsulfonyl group, or a C₁₋₆ alkyl group substituted by an amino group substituted by a C₂₋₄ alkylcarbonyl group,each of R^(a2) and R_(a3) which are independent of each other, is a hydrogen atom, a C₁₋₆ alkyl group, a mono-, di- or poly-halogeno C₁₋₆ alkyl group, a C₁₋₆ alkoxy group, a mono-, di or poly-halogeno C₁₋₆ alkoxy group, a C₁₋₆ alkylthio group, a C₁₋₆ alkylsulfinyl group, a C₁₋₆ alkylsulfonyl group, a C₂₋₇ alkoxycarbonyl group, a C₂₋₇ alkylcarbonyl group, a halogen atom, a nitro group, a cyano group, or a phenyl group (provided that such a phenyl group may be substituted by one or more substituents selected from the group consisting of a halogen atom, a trifluoromethyl group, a nitro group, a C₁₋₆ alkyl group, a C₁₋₆ alkoxy group and a C₂₋₇ alkoxycarbonyl group); X is an oxygen atom or a sulfur atom, L is a hydrogen atom, a C₁₋₆ alkyl group, a C₂₋₆ alkenyl group or a C₂₋₆ alkynyl group, G is ##STR1204## A is a nitrogen atom, and each of Z and D which are independent of each other, is a C₁₋₄ alkyl group, a C₁₋₄ alkoxy group, a mono-, di- or poly-halogeno C₁₋₄ alkyl group, a mono-, di- or poly-halogeno C₁₋₄ alkoxy group, a halogen atom, a C₁₋₄ alkylamino group or a di(C₁₋₃ alkyl)amino group.
 3. A herbicida composition comprising a compound according to claim 2 and an inert carrier.
 4. A method of controlling the growth of weeds, comprising applying to said weeds a herbicidally effective amount of a compound according to claim
 2. 5. The compound of claim 2, wherein the mono-, di- or poly-halogeno C₁₋₄ alkyl group is selected from the group consisting of a monochloro C₁₋₄ alkyl group, a di-chloro C₁₋₄ alkyl group, a poly-chloro C₁₋₄ alkyl group, a mono-fluoro C₁₋₄ alkyl group, a di-fluoro C₁₋₄ group, and a poly-fluoro C₁₋₄ alkyl group, and wherein said mono-, di- or poly-halogeno C₁₋₄ alkoxy group is selected from the group consisting of a monochloro C₁₋₄ alkoxy group, a dichloro C₁₋₄ alkoxy group, a polychloro C₁₋₄ alkoxy group, a monofluoro C₁₋₄ group, a difluoro C₁₋₄ alkoxy group and a polyfluoro C₁₋₄ alkoxy group. 